Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10202564 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
3217 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
CHEMBL362628 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
10202564 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
3217 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
CHEMBL362628 1496 8 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
6918836 60217 15 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
CHEMBL175835 60217 15 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
6918836 60217 15 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
CHEMBL175835 60217 15 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
16718917 181100 0 None 2290 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 181100 0 None 2290 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
16718920 189085 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
CHEMBL515307 189085 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
71459954 78772 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
CHEMBL2113386 78772 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
71459954 78772 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 78772 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
11234629 200527 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL609741 200527 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
16112801 180509 0 None 1258 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL476006 180509 0 None 1258 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
11463428 200067 0 None - 1 Human 9.0 pEC50 = 9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606639 200067 0 None - 1 Human 9.0 pEC50 = 9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
11200511 200045 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 200045 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
11280663 200558 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
CHEMBL609995 200558 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
11223004 200528 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 200528 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
11749539 200555 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
CHEMBL609992 200555 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
11451904 200608 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL610254 200608 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11210467 200523 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
CHEMBL609737 200523 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
11384146 200048 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 200048 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
44403084 71400 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196622 71400 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
23655289 88261 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL235986 88261 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
45484384 197189 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584049 197189 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
3245407 47841 23 None 1 6 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 47841 23 None 1 6 Human 6.0 pEC50 = 6.0 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
45484333 195141 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565724 195141 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
46880707 8453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1094370 8453 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
11333554 96213 19 None -64 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96213 19 None -64 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
25208878 180481 0 None 77 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL475969 180481 0 None 77 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc2C1 10.1021/jm8009469
23655287 88260 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
CHEMBL235985 88260 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
10067306 197188 0 None 8 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 197188 0 None 8 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
45484307 195154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565753 195154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403055 69504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193824 69504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435607 88707 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236576 88707 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
22028185 197362 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585931 197362 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435608 88710 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236577 88710 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435643 147066 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393107 147066 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23655462 89792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL238277 89792 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
10017687 66945 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL188182 66945 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
10472158 195150 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 195150 0 None -1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
11775364 200102 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 200102 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
23655468 88961 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236989 88961 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
14571158 148549 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL394303 148549 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
11211722 200050 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606558 200050 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
73354882 89263 1 None 14 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89263 1 None 14 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11363934 200557 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
CHEMBL609994 200557 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
11453792 200046 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606548 200046 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
45484381 196812 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
CHEMBL577687 196812 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
46880531 6222 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081793 6222 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
44435614 153913 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL399013 153913 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
73356442 89266 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376485 89266 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44435616 147321 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393312 147321 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9902533 133079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
CHEMBL371292 133079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
45484297 195620 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568672 195620 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44433197 88347 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236313 88347 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11709684 196940 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
CHEMBL578826 196940 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
11709684 196940 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL578826 196940 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44403064 133049 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371132 133049 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10380133 196659 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL576315 196659 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435635 88772 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236772 88772 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435604 154322 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL400627 154322 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484398 195192 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565977 195192 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435646 145027 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL391517 145027 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16718827 174836 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
CHEMBL457570 174836 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptorAgonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
11385064 200049 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606557 200049 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44435629 148162 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393997 148162 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484352 196959 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL579063 196959 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
44435641 147064 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393106 147064 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9999118 6092 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081094 6092 4 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
45484299 195541 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568249 195541 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45484322 197127 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL583389 197127 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
73351903 89265 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89265 0 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89268 0 None 32 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89268 0 None 32 4 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44433198 146580 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392746 146580 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403072 70066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194568 70066 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435610 88367 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236404 88367 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484399 197286 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585098 197286 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9902533 133079 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133079 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
12147013 65251 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL183203 65251 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
46880657 6302 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082198 6302 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
44435647 88081 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235117 88081 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880655 5477 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1076684 5477 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
11316594 200556 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
CHEMBL609993 200556 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
46227395 198445 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL596199 198445 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11351089 200051 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606559 200051 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
11440676 200529 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
CHEMBL609743 200529 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
44435637 88934 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236976 88934 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
5 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5202 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
CHEMBL39 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
DB08839 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT6 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2020.112709
5 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
5202 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
CHEMBL39 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
DB08839 139 66 None -181 27 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at serotonin 5-HT6R receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.8b01096
44435627 88072 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235070 88072 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45484382 195142 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
CHEMBL565730 195142 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
44435638 154389 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL401018 154389 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11200157 200078 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606705 200078 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
73347306 89264 0 None 15 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89264 0 None 15 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesAgonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11452988 200554 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
CHEMBL609991 200554 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptorEffective agonist concentration in cAMP release assay in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
44435653 146867 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392976 146867 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435628 147970 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393830 147970 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10407367 195118 0 None 10 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 195118 0 None 10 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44403059 123854 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363827 123854 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435613 153869 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398809 153869 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
23655469 88962 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236990 88962 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
46880486 6093 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081095 6093 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10199819 133085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371318 133085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
46880607 5897 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079977 5897 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
10150497 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
3240 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
CHEMBL392760 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
10150497 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
10150497 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
3240 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
CHEMBL392760 4011 41 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassayAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
73350387 89267 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89267 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Partial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutesPartial agonist activity at human 5HT6 receptor expressed in BHK cells assessed as stimulation of cAMP production after 45 minutes
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
9840311 5475 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076665 5475 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
44435642 88209 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235734 88209 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11725505 197361 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585930 197361 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
44433196 88294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236104 88294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10177537 123857 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363843 123857 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435649 145292 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL391713 145292 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23625764 146772 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL392899 146772 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880608 5943 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080316 5943 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10337743 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
8429 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
CHEMBL571858 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
10337743 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 4013 16 None 47 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
44435652 88824 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236812 88824 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435639 88120 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235306 88120 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880529 6094 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
CHEMBL1081110 6094 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
21071574 123565 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL363275 123565 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
44433193 88293 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236103 88293 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10042892 5457 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076583 5457 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAgonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as effect on 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
45484383 195143 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565731 195143 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIAAgonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
44403096 71784 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
CHEMBL197845 71784 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptorsEffective concentration for cAMP production in HeLa cells expressing human 5-HT6 receptors
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
23655465 88958 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL236987 88958 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAgonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
44435650 88082 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235118 88082 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAgonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
11361090 63974 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181066 63974 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
11624561 69944 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL187865 69944 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL194307 69944 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44389001 63470 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180221 63470 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
11396708 200525 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
CHEMBL609739 200525 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
11524473 134316 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL371886 134316 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
11739679 169285 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL444015 169285 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
44403044 161162 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL413525 161162 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
11282884 200610 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
CHEMBL610256 200610 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
44389081 62324 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178385 62324 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
49836923 18576 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277918 18576 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554395 18536 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18536 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
11201726 200613 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
CHEMBL610259 200613 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
49836825 18535 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
CHEMBL1277564 18535 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
49836826 18545 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277656 18545 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44389004 122610 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL361180 122610 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
49836827 18554 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277751 18554 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836828 18562 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277836 18562 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
44554394 18546 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277657 18546 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44433195 146352 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392541 146352 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263302 191387 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191387 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
46189984 68548 1 None - 1 Human 8.0 pIC50 = 8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68548 1 None - 1 Human 8.0 pIC50 = 8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
11316095 200103 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606817 200103 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
162676953 182940 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4799851 182940 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
24784575 176140 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
CHEMBL459989 176140 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
21071390 1956 48 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
8689 1956 48 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
CHEMBL3286580 1956 48 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
DB11957 1956 48 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
18590409 10554 9 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170463 10554 9 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
46224917 197790 5 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591570 197790 5 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 306 2 0 2 4.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
49836615 18601 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1278091 18601 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
52918031 57361 3 None - 1 Human 7.0 pIC50 = 7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57361 3 None - 1 Human 7.0 pIC50 = 7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
24763349 62301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783608 62301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
16070169 59779 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642850 59779 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739214 59779 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53320775 59813 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642878 59813 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739546 59813 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
58357671 128514 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670291 128514 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 365 4 1 7 2.7 CNc1nn2c(-c3cccnc3)ccnc2c1S(=O)(=O)c1ccccc1 nan
54582939 62392 6 None -8 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783957 62392 6 None -8 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 369 3 0 3 4.0 CN1CCc2c(c3cc(Br)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901255 10853 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173281 10853 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 3 0 9 2.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCOCC1)c1sccc12 10.1016/j.bmc.2010.05.051
24783809 176139 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459988 176139 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
16019451 10887 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173570 10887 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 7 1 8 4.4 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
44126270 197472 6 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589389 197472 6 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 4 0 3 3.9 COc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
54585846 62398 4 None -38 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
CHEMBL1783963 62398 4 None -38 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 323 3 0 3 3.7 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cn1 10.1016/j.bmcl.2009.04.128
46880606 5896 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1079976 5896 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
46880756 5950 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080380 5950 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10136185 126658 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365753 126658 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
20901273 10541 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170291 10541 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 509 4 1 8 5.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
24763430 62290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783582 62290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
49836617 18616 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278180 18616 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
18560541 10833 10 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173061 10833 10 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.2 CC(Cc1ccccc1)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512797 142324 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3893286 142324 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 403 7 1 4 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc(Cl)c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
44435625 148466 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL394233 148466 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
25263297 183755 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 183755 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
4106 2466 16 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2466 16 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2466 16 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2466 16 None -29 7 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
44403048 132184 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL369910 132184 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
44388950 122089 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL360234 122089 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
46189932 68543 3 None - 1 Human 8.0 pIC50 = 8.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68543 3 None - 1 Human 8.0 pIC50 = 8.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53259021 69404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69404 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
16019576 10796 6 None 1995 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10796 6 None 1995 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
18591269 10865 2 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173362 10865 2 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10115005 71340 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196466 71340 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10117854 126903 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL366012 126903 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
18560059 10808 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172791 10808 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 0 8 4.8 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18559283 10555 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170464 10555 9 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 5 1 8 5.7 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
53324933 57317 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668502 57317 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
49836621 18468 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276926 18468 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
44403047 167864 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL434932 167864 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
16019286 10846 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173206 10846 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
46225001 197437 4 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589149 197437 4 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 326 3 0 2 4.2 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
18560559 10581 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170682 10581 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16804502 10585 13 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170686 10585 13 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 471 5 1 9 4.6 COc1ccccc1Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
18560180 10535 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170276 10535 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
197033 197473 58 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 197473 58 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
24783550 176158 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460194 176158 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
16019548 10781 9 None 23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172597 10781 9 None 23 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(Cl)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
44156502 60659 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762569 60659 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 nan
16117278 59833 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642884 59833 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739659 59833 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18590273 10677 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171632 10677 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117151 59771 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 59771 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 59771 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
56655504 68527 2 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68527 2 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849579 68532 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922619 68532 3 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357768 128516 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670293 128516 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 395 5 1 8 2.7 CNc1nn2c(OC)cc(-c3cccnc3)nc2c1S(=O)(=O)c1ccccc1 nan
25123014 198747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 198747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44435624 88674 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236541 88674 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24784573 175614 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459348 175614 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
49798859 10467 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169724 10467 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccc(Cl)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
7185128 10873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173433 10873 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901271 10559 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170472 10559 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)cc1 10.1016/j.bmc.2010.05.051
20901291 10662 5 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1171486 10662 5 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 7 1 8 4.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
16019607 10827 3 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173005 10827 3 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 0 8 3.7 CCN(CC)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901207 10882 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10882 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
10202995 70209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194786 70209 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
16117281 59828 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642880 59828 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739648 59828 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16019305 10481 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169898 10481 8 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 5 1 10 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc4c(c2)OCO4)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799667 10812 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10812 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
16117282 59822 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642888 59822 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739615 59822 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
4106 2466 16 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
5358812 2466 16 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
89 2466 16 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
CHEMBL93240 2466 16 None -29 7 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2007.11.045
20901220 10817 4 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172868 10817 4 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16071727 59786 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642848 59786 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739253 59786 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
10430623 18488 22 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18488 22 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
9950402 169886 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL444878 169886 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435623 148465 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394232 148465 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
49836509 18584 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277999 18584 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
57402070 71219 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71219 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71219 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
18560325 10856 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173284 10856 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
49799664 10898 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173774 10898 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(C2CCN(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44435612 88368 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236405 88368 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57396850 71180 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71180 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71180 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
24965679 83621 13 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207386 83621 13 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
18590416 10588 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170689 10588 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)cc1C 10.1016/j.bmc.2010.05.051
57393365 71206 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
53325577 59842 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642874 59842 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739700 59842 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
18560539 10779 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172595 10779 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18560202 10533 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170274 10533 11 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16117279 59820 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 59820 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 59820 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
11316536 200094 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606765 200094 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
44388951 62200 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178234 62200 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
563919 98821 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL281937 98821 4 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
20901117 10576 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10576 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019610 10763 10 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172404 10763 10 None 50 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 4 1 8 5.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
71769424 91523 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414704 91523 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 551 6 0 7 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c(N(C)C)cccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
118727447 116935 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
CHEMBL3398395 116935 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 459 8 0 9 2.7 COc1ccc(OC)c(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)c1 10.1016/j.bmc.2015.01.032
44435619 88355 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236335 88355 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118512792 144588 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3911908 144588 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 420 7 1 5 4.1 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
18591074 10793 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172723 10793 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2ccc(Cl)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
46224941 197470 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589386 197470 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
18560060 10807 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172790 10807 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 0 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N(C)Cc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7184895 10551 7 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170439 10551 7 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 6 1 9 2.5 COCCNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16118795 59780 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 59780 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 59780 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
86302554 110344 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110344 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
45484298 195621 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568673 195621 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
45113400 14116 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099284 14116 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199172 14116 2 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
10291754 70091 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL194590 70091 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
25067564 199615 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 199615 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
20901261 10578 7 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170679 10578 7 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
20901266 10810 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172793 10810 8 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
20901268 10899 5 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173777 10899 5 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 437 7 1 9 3.3 COCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224944 197896 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL592516 197896 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 336 3 0 3 4.4 COc1ccc(/C=C\n2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
16019510 10896 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173706 10896 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 3 0 8 3.8 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
23652787 56394 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642419 56394 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
20901258 10847 3 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173207 10847 3 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(N1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
56849580 68533 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922620 68533 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318111 59772 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642862 59772 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739117 59772 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53318268 57356 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668582 57356 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
25117680 198951 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 198951 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
7184976 10635 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171092 10635 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54586812 62388 4 None -12 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783953 62388 4 None -12 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
42631003 197937 10 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 197937 10 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
16718922 196543 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
CHEMBL575310 196543 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
54582940 62393 4 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783958 62393 4 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
16117153 59823 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 59823 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 59823 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
53324896 57359 3 None - 1 Human 7.8 pIC50 = 7.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668585 57359 3 None - 1 Human 7.8 pIC50 = 7.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
25123013 198774 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 198774 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
44155109 8090 3 None 21 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8090 3 None 21 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46227396 199955 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 199955 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
16019453 10838 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173127 10838 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 5 1 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24894055 182586 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL479548 182586 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMPAntagonist activity at cloned human 5HT6 receptor expressed in HeLa cells assessed as production of cAMP
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
18590411 10822 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172938 10822 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 493 5 1 9 3.5 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
71813838 91159 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407545 91159 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 430 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(Cl)c4C)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
46224880 199186 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL601304 199186 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 304 2 0 2 4.3 Cc1ccc2c(c1)C1CN(C)CCC1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
71695200 129240 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129240 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44388970 64525 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182099 64525 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880708 7365 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1086719 7365 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
49836823 18523 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
CHEMBL1277466 18523 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
23655467 88960 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
CHEMBL236988 88960 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
25117677 198568 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 198568 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
126720440 162476 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175829 162476 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
24771124 183752 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484333 183752 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019580 10463 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10463 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16019288 10591 7 None 234 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170696 10591 7 None 234 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 433 4 1 8 4.2 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019550 10607 14 None 131 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170886 10607 14 None 131 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.3 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901217 10806 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172789 10806 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
56849581 68534 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68534 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
56849715 68537 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922624 68537 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16118796 59782 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642853 59782 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739217 59782 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
18559973 10537 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170280 10537 9 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.8 CCc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224918 197812 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591801 197812 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 2 0 2 4.1 CN1CCC2C(C1)c1cc(F)ccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
45483622 196414 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574403 196414 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
52918030 57343 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668569 57343 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
129103318 166760 0 None -19 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 166760 0 None -19 6 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
118512804 157122 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
CHEMBL4081529 157122 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 438 7 1 5 4.2 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3cccnc23)nn1-c1ccc(F)cc1 10.1016/j.bmcl.2017.07.031
23653062 56399 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642424 56399 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
57396848 71192 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71192 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71192 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
46880532 6223 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081794 6223 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
16019609 10512 10 None 223 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170098 10512 10 None 223 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 8 4.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)c2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
46224914 197865 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592271 197865 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.7 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
71769065 91526 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414711 91526 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 458 5 0 6 4.1 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
20901172 10483 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169900 10483 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 497 6 1 8 5.6 CC(C)c1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
118727442 116930 0 None -5 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398389 116930 0 None -5 2 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 399 6 0 7 2.7 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccccc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
56849581 68534 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922621 68534 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44435615 88711 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236578 88711 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
53319627 57355 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668581 57355 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
53323599 57349 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668575 57349 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
53320009 56369 0 None 2 7 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56369 0 None 2 7 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
53323402 59826 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642864 59826 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739646 59826 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117283 59832 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1642883 59832 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1739658 59832 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
3232 3453 13 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
3248571 3453 13 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
CHEMBL60264 3453 13 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1016/j.bmcl.2013.05.100
53326177 57362 3 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57362 3 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
44388931 63783 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180826 63783 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
7185122 10508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170093 10508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 389 6 1 9 2.2 COCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901254 10809 8 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172792 10809 8 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
7470702 10552 9 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170442 10552 9 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 0 8 3.6 CCc1ccc(S(=O)(=O)c2nnn3c2nc(N(CC)CC)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
16019490 10897 4 None 8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173709 10897 4 None 8 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 3 0 9 2.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCOCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
18590413 10880 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173503 10880 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 0 8 4.6 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16222547 81626 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165541 81626 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
45487150 196043 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL571413 196043 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
56849714 68536 4 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922623 68536 4 None - 1 Human 6.7 pIC50 = 6.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46224945 199721 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL604669 199721 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 5.0 C/C(=C/c1ccccc1)n1c2c(c3cc(C)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49799663 10574 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170664 10574 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 3 0 8 4.0 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N2CCC(C)CC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
20901114 10839 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
CHEMBL1173132 10839 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 442 4 1 9 1.9 NC(=O)C1CCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)CC1 10.1016/j.bmc.2010.05.051
131999484 182021 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182021 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182021 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
49836924 18586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
CHEMBL1278000 18586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
44156626 57364 3 None - 1 Human 8.7 pIC50 = 8.7 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668590 57364 3 None - 1 Human 8.7 pIC50 = 8.7 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44554228 18555 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277752 18555 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44389016 63589 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180606 63589 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
11256720 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
9444 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
CHEMBL1083390 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
DB12680 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
11256720 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
11256720 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
9444 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL1083390 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
DB12680 2024 73 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assayInverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
49836824 18524 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277467 18524 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44554227 18563 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18563 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
135398737 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
38 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
722 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
CHEMBL42 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
DB00363 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.8b01096
135398737 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
38 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
722 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
CHEMBL42 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
DB00363 944 89 None -12 36 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.112709
7185123 10577 7 None 851 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10577 7 None 851 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
20901267 10845 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1173205 10845 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 3 0 8 4.1 CC1CCCN(c2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
16019602 10587 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170688 10587 5 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 4 1 8 5.3 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4ccc(Br)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
25117681 198872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599023 198872 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
20901132 10742 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172207 10742 3 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 4 1 8 3.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18560542 10805 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
CHEMBL1172788 10805 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 413 3 0 8 3.4 CC1CCCN(c2nc3c(S(=O)(=O)c4ccccc4)nnn3c3ccsc23)C1 10.1016/j.bmc.2010.05.051
71770944 91533 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
CHEMBL2414732 91533 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2013.05.051
71770944 91533 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
CHEMBL2414732 91533 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 446 4 0 6 3.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2015.01.032
16222549 81608 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165524 81608 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
54583938 62404 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783970 62404 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 306 3 0 4 3.0 Cc1ccc2c(c1)c1c(n2CCc2cnccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
46225002 197813 4 None -602 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL591803 197813 4 None -602 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 376 3 0 2 5.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
16116900 59785 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642847 59785 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739252 59785 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
57398718 69402 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69402 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
118173755 191736 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206617 191736 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
10141477 139728 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380556 139728 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
11177383 200047 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606549 200047 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
46227404 198201 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL594548 198201 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
11235953 200101 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606815 200101 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
118727445 116933 0 None -8 3 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398392 116933 0 None -8 3 Human 5.7 pIC50 = 5.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 413 6 0 7 3.0 Cc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
44435617 88712 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236579 88712 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
20901163 10874 8 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173434 10874 8 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 423 6 1 9 2.9 COCCNc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
58357790 129244 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3675195 129244 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 2 7 1.5 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
16019312 10797 0 None 144 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172727 10797 0 None 144 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 5 1 9 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
58357705 128508 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
CHEMBL3670284 128508 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(C)c1 nan
20901131 10468 7 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1169725 10468 7 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1cccc(CNc2nc3c(S(=O)(=O)c4ccc(C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
49799645 10794 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172724 10794 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 4 1 8 5.5 Cc1cc(Cl)cc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
57403833 71126 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71126 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71126 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44126328 199420 4 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL603049 199420 4 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
68303508 129241 4 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675192 129241 4 None - 1 Human 5.6 pIC50 = 5.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
53323439 59841 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642873 59841 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739699 59841 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44435621 88356 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236336 88356 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24965329 83623 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207388 83623 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human 5HT6 receptor expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
46225027 197438 4 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589150 197438 4 None -74 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 338 4 0 3 4.0 COc1ccc(CCn2c3c(c4cc(F)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44474625 13957 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197521 13957 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL575270 13957 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
20901145 10709 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1171992 10709 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 431 7 1 9 3.2 COCCCNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322935 57363 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668589 57363 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
44403103 140778 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL383373 140778 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44263496 199840 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL605292 199840 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by HTRF assay
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
71770821 91530 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414725 91530 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 474 5 0 7 3.7 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(C)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
118512815 151145 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3964100 151145 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2cccc3ccccc23)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
118727448 116936 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
CHEMBL3398396 116936 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 463 7 0 8 3.4 COc1ccc(Cl)cc1S(=O)(=O)n1cc(/C=N/N=C/N(C)C)c2c([N+](=O)[O-])cccc21 10.1016/j.bmc.2015.01.032
57403837 71129 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71129 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71129 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
24783810 175623 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459371 175623 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
10274389 132901 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370507 132901 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46189987 68547 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1922634 68547 2 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11775364 200102 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 200102 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptorInhibition of 5-HT stimulated cAMP production in HeLa cells expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
20901128 10848 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173208 10848 2 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 5 1 9 3.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
18591272 10560 9 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170473 10560 9 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 459 4 1 8 4.7 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
16750338 62300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783607 62300 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
118727450 116938 0 None -5 3 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398398 116938 0 None -5 3 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc3ccccc3c2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
46224878 197788 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
CHEMBL591568 197788 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 290 2 0 2 4.0 CN1CCC2C(C1)c1ccccc1N2/C=C/c1ccccc1 10.1016/j.bmcl.2009.11.037
44433194 146069 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392318 146069 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11545169 147118 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393158 147118 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263299 191520 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520343 191520 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
21071390 1956 48 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
8689 1956 48 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
CHEMBL3286580 1956 48 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
DB11957 1956 48 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
46190034 68549 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922636 68549 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
25122652 198978 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 198978 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
25263301 184036 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484927 184036 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
16019601 10464 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169708 10464 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901120 10534 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170275 10534 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 403 7 1 9 2.6 COCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799683 10840 3 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173135 10840 3 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 422 5 1 9 3.2 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
45113275 9019 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099282 9019 6 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 293 2 1 3 1.4 CN1CCc2[nH]c3ccc(S(=O)(=O)N(C)C)cc3c2C1 10.1016/j.ejmech.2009.10.035
16117280 59821 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642887 59821 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739614 59821 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
57393363 71220 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71220 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71220 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
44156863 7995 0 None 21 2 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 7995 0 None 21 2 Human 7.6 pIC50 = 7.6 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
16019372 10580 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170681 10580 8 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
44126269 199799 4 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 199799 4 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44435631 89247 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237594 89247 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122651 198565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 198565 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
18560562 10513 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170099 10513 9 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 1 8 5.0 CC(Nc1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
45113535 14125 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1097614 14125 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
CHEMBL1199305 14125 1 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 480 4 0 6 4.0 Cc1ccc(S(=O)(=O)n2c3c(c4cc(S(=O)(=O)c5ccccc5)ccc42)CN(C)CC3)cc1 10.1016/j.ejmech.2009.10.035
57403835 71127 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949767 71127 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962397 71127 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
46224915 197894 3 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592514 197894 3 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 370 2 0 2 5.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
18591268 10798 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172728 10798 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118173772 189781 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5177311 189781 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
20901118 10462 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169706 10462 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 10 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
18560182 10762 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172403 10762 8 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 451 6 1 9 3.8 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
71769190 91528 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414713 91528 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 476 5 0 6 4.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
23624297 56388 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642413 56388 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
45487139 195664 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL568935 195664 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
46224942 199720 3 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL604668 199720 3 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 324 2 0 2 4.5 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(F)cc2)C1 10.1016/j.bmcl.2009.11.037
118727449 116937 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398397 116937 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 449 6 0 7 3.9 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2cccc3ccccc23)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54579956 62391 4 None -3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783956 62391 4 None -3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
53326176 57360 3 None - 1 Human 8.5 pIC50 = 8.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57360 3 None - 1 Human 8.5 pIC50 = 8.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
10405986 18602 1 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1278092 18602 1 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
57396970 69400 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69400 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
118181460 189301 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5169546 189301 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44327759 206175 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL96745 206175 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
16071847 59829 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 59829 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 59829 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44389002 63233 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180066 63233 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
53318109 59787 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642849 59787 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739254 59787 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
18560186 10482 9 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169899 10482 9 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 0 8 4.5 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10356663 111451 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111451 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
58357851 128504 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670280 128504 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357730 128510 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
CHEMBL3670286 128510 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 412 5 0 8 3.4 COc1cc(-c2ccccn2)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 nan
57398615 71205 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71205 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71205 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
44389074 122796 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361572 122796 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
71814157 91163 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407553 91163 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2013.05.100
71814318 91164 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
CHEMBL2407554 91164 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 439 5 3 5 2.4 O=C1c2[nH]nc(NS(=O)(=O)c3ccc4ccccc4c3)c2CCN1CC1CCNCC1 10.1016/j.bmcl.2017.07.031
23653135 56387 3 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642412 56387 3 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
25117679 198920 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 198920 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
57400392 69410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69410 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
18560181 10611 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170892 10611 10 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 8 4.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1Cl)c1sccc12 10.1016/j.bmc.2010.05.051
44155109 8090 3 None 21 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8090 3 None 21 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
10356663 111451 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL328816 111451 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
53322548 56393 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642418 56393 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometryAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
54580942 62402 9 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783967 62402 9 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 309 3 0 3 3.4 CN1CCc2c(c3cc(F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
71813833 91157 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407540 91157 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 450 4 2 4 3.7 Cc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(C(F)(F)F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
57391618 71125 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71125 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71125 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
25122654 198844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 198844 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
44388944 62689 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178767 62689 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
118512805 147031 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3930881 147031 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 419 7 1 4 4.7 CC(C)Cc1cc(CNS(=O)(=O)c2ccc3ccccc3c2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836715 18475 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277010 18475 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
44435633 89111 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237389 89111 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57391729 69403 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69403 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
16019553 10606 7 None 912 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10606 7 None 912 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44435609 153868 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398808 153868 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
45113404 14107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095273 14107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199078 14107 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 327 2 1 4 2.4 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccnc4)cc3c2C1 10.1016/j.ejmech.2009.10.035
58357665 128515 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670292 128515 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(-c3cccnc3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
164622805 185281 0 None -30 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185281 0 None -30 6 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
44155107 7996 3 None 60 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 7996 3 None 60 2 Human 7.5 pIC50 = 7.5 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16019339 10504 5 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170087 10504 5 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 4 1 8 4.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
16019508 10811 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172794 10811 6 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
57395082 71200 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949766 71200 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963006 71200 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57520121 72920 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
CHEMBL2012637 72920 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2012.02.020
57520121 72920 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
CHEMBL2012637 72920 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 374 5 1 5 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3snc(/N=C/N(C)C)c3c2)cc1 10.1016/j.bmc.2015.01.032
73347610 91524 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414705 91524 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 462 5 0 8 2.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3nccn3C)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
60141574 72921 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012639 72921 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 394 5 1 5 4.0 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc12 10.1016/j.bmc.2012.02.020
18560538 10503 9 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1170086 10503 9 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 5 1 8 4.3 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
621659 62400 10 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783965 62400 10 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
7184886 10506 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10506 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224973 197936 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
CHEMBL592751 197936 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 320 2 0 2 4.8 C/C(=C/c1ccccc1)n1c2c(c3cc(F)ccc31)CN(C)CC2 10.1016/j.bmcl.2009.11.037
49836620 18467 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276925 18467 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
45378935 197824 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591939 197824 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
73349123 91525 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414707 91525 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 516 5 0 8 3.9 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4c3OCCO4)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
18590836 10466 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1169722 10466 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 4 1 8 4.4 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(F)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
45487129 196129 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL572092 196129 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
25117676 198775 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 198775 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
135339817 180902 0 None -6 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 180902 0 None -6 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
45113401 9021 1 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
CHEMBL1099285 9021 1 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 435 5 2 3 4.7 O=S(=O)(Nc1cccc(F)c1)c1ccc2[nH]c3c(c2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2009.10.035
118727451 116939 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
CHEMBL3398399 116939 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3ccc(NS(=O)(=O)c4cccc5ccccc45)cc3s2)CC1 10.1016/j.bmc.2015.01.032
10286610 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL355905 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assayAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52918032 57338 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668564 57338 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 nan
53322258 57339 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668565 57339 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357784 128513 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670290 128513 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 379 4 1 7 3.0 CNc1nn2c(C)cc(-c3ccncc3)nc2c1S(=O)(=O)c1ccccc1 nan
53326178 57370 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668596 57370 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
44389023 62186 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
CHEMBL178193 62186 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
44554393 18361 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18361 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
4106 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting methodAgonist activity at human 5-HT6 receptor expressed in CHOK1 cells assessed as calcium mobilization by radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
4106 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2466 16 None -29 7 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT6 receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
57400234 71196 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71196 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71196 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
49836716 18476 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1277011 18476 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
7184883 10795 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10795 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
118512841 155915 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
CHEMBL4067243 155915 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 417 7 1 4 4.5 Cc1c(Cl)cccc1S(=O)(=O)NCc1cc(CC(C)C)n(-c2ccccc2)n1 10.1016/j.bmcl.2017.07.031
44126327 199968 4 None -41 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL606036 199968 4 None -41 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 372 3 0 2 5.2 Cc1ccc2c(c1)c1c(n2CCc2ccc(C(F)(F)F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
45487128 196110 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571878 196110 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
18560556 10816 11 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172867 10816 11 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 445 5 1 9 4.0 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
53320926 57341 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1668567 57341 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 nan
9929294 63749 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180765 63749 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44388999 63051 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179592 63051 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
10115854 69256 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193450 69256 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
54581998 62406 4 None -5 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783972 62406 4 None -5 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 368 4 0 4 4.3 CN1CCc2c(c3cc(-c4cccnc4)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
45378936 197825 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 197825 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
54581997 62401 6 None -11 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783966 62401 6 None -11 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccncc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
16117152 59770 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642885 59770 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739101 59770 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
44126330 62395 4 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783960 62395 4 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2cccnc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
57520122 72922 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
CHEMBL2012643 72922 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetryAntagonist activity at human recombinant 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5HT-induced intracellular calcium level incubated for 15 mins prior to 5HT-induction measured after 1 hr by fluo-4-AM-based fluorimetry
ChEMBL 410 5 1 5 4.5 CN(C)/C=N/c1nsc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1016/j.bmc.2012.02.020
45378934 199961 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 199961 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
57396813 71201 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None 39 4 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
53323601 57367 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57367 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
46189980 68552 2 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68552 2 None - 1 Human 7.4 pIC50 = 7.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
21254909 57316 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668501 57316 2 None - 1 Human 6.4 pIC50 = 6.4 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53318142 59774 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642867 59774 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739135 59774 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16049388 81611 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165527 81611 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
20901141 10608 5 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170887 10608 5 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
10068007 18600 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278090 18600 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
44474631 13968 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197618 13968 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL578631 13968 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
7246142 10821 9 None 85 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172934 10821 9 None 85 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.6 CC(C)Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901139 10854 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173282 10854 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)c(C)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53320927 57344 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668570 57344 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
71770822 91531 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
CHEMBL2414726 91531 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 414 4 0 6 2.9 Cc1c(/C=N/N2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2013.05.051
46884709 7997 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 7997 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
16116898 59812 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1642877 59812 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1739545 59812 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
18591271 10557 12 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170466 10557 12 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 473 5 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901160 10815 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172866 10815 6 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 5 1 9 3.4 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
44403097 72101 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198827 72101 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44435644 88700 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236571 88700 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
118727443 116931 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398390 116931 0 None -7 2 Human 5.3 pIC50 = 5.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 417 6 0 7 2.8 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(F)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
44516817 57358 4 None 1023 2 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668584 57358 4 None 1023 2 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44156624 57365 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668591 57365 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
162646407 179043 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4742804 179043 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
45484340 195151 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565746 195151 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
162656068 180234 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756814 180234 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
44435603 91318 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL240922 91318 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435640 154390 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL401019 154390 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
49799684 10841 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173136 10841 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 436 5 0 9 3.2 CN(Cc1cccnc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901125 10875 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173435 10875 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 5 1 9 3.7 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
6625986 10505 10 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170088 10505 10 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 407 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
25123012 200024 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
CHEMBL606401 200024 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
126720394 161764 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164541 161764 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357663 128507 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670283 128507 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 426 5 0 8 4.1 CSc1nn2c(C)c(Oc3cccnc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357754 128511 3 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670288 128511 3 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
9924959 69121 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193358 69121 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
16019364 10855 5 None 53 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173283 10855 5 None 53 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 467 5 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
53318300 57314 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668499 57314 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
71813685 91165 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407562 91165 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 400 4 2 4 2.9 Cc1ccc(N2CCc3c(NS(=O)(=O)c4ccc(F)cc4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
18559939 10532 12 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170273 10532 12 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
24794436 13955 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL1197511 13955 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL574856 13955 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
25263300 184035 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484926 184035 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
10136837 165410 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
CHEMBL425196 165410 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
10136837 165410 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL425196 165410 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44474797 13950 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL1197505 13950 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574625 13950 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
49836508 18583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
CHEMBL1277998 18583 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
57402187 69407 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69407 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
20901263 10579 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170680 10579 5 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956087 10879 10 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
CHEMBL1173502 10879 10 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 513 5 1 8 5.1 CC(Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12)c1ccccc1 10.1016/j.bmc.2010.05.051
49836619 18457 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276839 18457 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
46224916 197789 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL591569 197789 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 332 3 0 3 4.6 COc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
46224943 197895 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592515 197895 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 374 2 0 2 5.4 CN1CCc2c(c3cc(F)ccc3n2/C=C\c2ccc(C(F)(F)F)cc2)C1 10.1016/j.bmcl.2009.11.037
53319441 59783 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642845 59783 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739231 59783 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
44435622 88671 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236540 88671 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44403099 132489 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370215 132489 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
126720425 161565 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161308 161565 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
58357826 129245 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL3675196 129245 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 377 5 1 7 2.1 CNc1nn2c(C)cc(CN(C)C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
118512827 145898 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3921947 145898 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 437 7 1 4 4.9 CC(C)Cc1cc(CNS(=O)(=O)c2c(Cl)cccc2Cl)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
49836618 18456 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276838 18456 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
18560564 10514 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170100 10514 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 6 0 8 4.9 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Cl)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46224877 199017 5 None -74 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL599913 199017 5 None -74 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 288 2 0 2 4.3 CN1CCc2c(c3ccccc3n2/C=C\c2ccccc2)C1 10.1016/j.bmcl.2009.11.037
23725134 13940 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL1197475 13940 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL573521 13940 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
71813986 91160 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407547 91160 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 416 5 2 5 2.6 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(F)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
20901126 10465 7 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169709 10465 7 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 6 1 9 4.1 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(C)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16956089 10792 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172722 10792 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 527 6 0 8 5.0 CCN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
7184892 10835 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173063 10835 9 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 6 1 8 3.9 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
49799656 10872 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10872 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10872 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
54584885 62397 4 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783962 62397 4 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44474470 13947 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL1197489 13947 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL573981 13947 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
16019546 10610 6 None 676 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170891 10610 6 None 676 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 5 1 8 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901133 10536 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170279 10536 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 4 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(Nc2cccc(C)c2C)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901186 10538 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170281 10538 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 5 1 8 5.3 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019514 10765 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172406 10765 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.1 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC2CCCC2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
44224259 62394 4 None -30 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783959 62394 4 None -30 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2cccnc2)C1 10.1016/j.bmcl.2009.04.128
44155109 8090 3 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1091919 8090 3 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
57400234 71196 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71196 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71196 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
44156863 7995 0 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 7995 0 None 21 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
44156622 57366 3 None - 1 Human 8.2 pIC50 = 8.2 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668592 57366 3 None - 1 Human 8.2 pIC50 = 8.2 Functional
Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Lance cAMP Assay: Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
10449488 195191 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565976 195191 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
118181414 190601 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5189271 190601 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
126720397 180513 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760105 180513 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
162644347 181177 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4777550 181177 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Neutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assayNeutral antagonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as inhibition of WAY181187-induced cAMP accumulation by BRET assay
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
57393468 69409 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69409 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
46880757 5951 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080381 5951 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
20901264 10863 8 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173360 10863 8 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 421 6 1 8 4.0 CCCCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901122 10486 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1169903 10486 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 425 4 1 8 4.1 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
18560317 10814 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1172862 10814 10 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 483 5 1 8 5.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccccc2Cl)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
68261572 129242 4 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675193 129242 4 None - 1 Human 5.2 pIC50 = 5.2 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
10140915 139825 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380772 139825 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
20901229 10881 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173506 10881 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 409 2 1 8 2.5 Nc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
11595209 94400 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253708 94400 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassayAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-stimulated cAMP accumulation after 20 mins by enzyme-immunoassay
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
49836616 18615 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278179 18615 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
45113534 14113 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1097613 14113 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199141 14113 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 431 5 0 5 4.1 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2CCc2ccccn2)C1 10.1016/j.ejmech.2009.10.035
45113399 9020 3 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
CHEMBL1099283 9020 3 None - 1 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 348 2 1 4 1.1 CN1CCN(S(=O)(=O)c2ccc3[nH]c4c(c3c2)CN(C)CC4)CC1 10.1016/j.ejmech.2009.10.035
57391567 71193 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71193 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71193 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
20901115 10862 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10862 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
118727444 116932 0 None -25 2 Human 5.2 pIC50 = 5.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
CHEMBL3398391 116932 0 None -25 2 Human 5.2 pIC50 = 5.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 525 6 0 7 3.3 CN(C)/C=N/N=C/c1cn(S(=O)(=O)c2ccc(I)cc2)c2cccc([N+](=O)[O-])c12 10.1016/j.bmc.2015.01.032
54585847 62403 6 None -29 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783968 62403 6 None -29 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 359 3 0 3 4.3 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
44435626 154319 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
CHEMBL400608 154319 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
16019397 10857 11 None 54 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173286 10857 11 None 54 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 461 5 1 9 4.5 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
71769315 91529 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
CHEMBL2414722 91529 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 508 5 0 6 5.3 CN1CCN(/N=C/c2c(-c3ccccc3)n(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1016/j.bmc.2013.05.051
44126325 197435 4 None -10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL589147 197435 4 None -10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 334 4 0 3 4.2 COc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
57396813 71201 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None 39 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
20901210 10818 4 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172869 10818 4 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 463 6 1 8 4.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
71813835 91158 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
CHEMBL2407542 91158 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 412 5 2 5 2.7 COc1cccc(S(=O)(=O)Nc2n[nH]c3c2CCN(c2ccc(C)cc2)C3=O)c1 10.1016/j.bmcl.2013.05.100
20901259 10864 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173361 10864 5 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 435 6 1 8 4.3 CC(C)CCNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57393467 69405 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935595 69405 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
18560324 10609 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170890 10609 8 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 477 6 1 8 4.8 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)Cc2ccccc2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
44435630 89246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL237593 89246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
7185121 10507 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170092 10507 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 387 6 1 8 3.4 CCCCNc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
20901265 10634 7 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1171041 10634 7 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
126720403 162060 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162060 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assayAntagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
16019574 10780 10 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172596 10780 10 None 14 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccc(F)cc1)c1sccc12 10.1016/j.bmc.2010.05.051
20901253 10820 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1172933 10820 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 365 2 1 8 2.4 Nc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
46225000 197436 4 None -9 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589148 197436 4 None -9 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 308 3 0 2 4.0 CN1CCc2c(c3cc(F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
118181454 189368 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5170650 189368 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysisAntagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
9969402 70203 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194750 70203 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44403104 72134 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198941 72134 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44155107 7996 3 None 60 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 7996 3 None 60 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
44537940 18587 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18587 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
44403065 165759 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL427184 165759 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
46830134 8133 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8133 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
46830134 8133 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8133 0 None 37 2 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.Functional Assay: Compounds of general formulas 1 and 2 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin.
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44435632 89039 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237179 89039 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25122653 198843 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 198843 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
71813988 91161 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
CHEMBL2407549 91161 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 428 6 2 6 2.4 COc1ccc(N2CCc3c(NS(=O)(=O)c4cccc(OC)c4)n[nH]c3C2=O)cc1 10.1016/j.bmcl.2013.05.100
16019519 10866 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173364 10866 5 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
58357699 128512 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670289 128512 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 442 5 1 8 3.7 CNc1nn2c(-c3ccccn3)cc(-c3ccccn3)nc2c1S(=O)(=O)c1ccccc1 nan
53316984 57342 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668568 57342 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
16019303 10500 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1170069 10500 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 427 4 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
20901275 10561 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170474 10561 6 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1ccc(C)c(Nc2nc3c(S(=O)(=O)c4cccc(Cl)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
16019310 10659 10 None 47 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1171436 10659 10 None 47 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 453 5 1 8 4.2 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccc(F)cc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
71815503 116934 0 None -3 3 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
CHEMBL3398394 116934 0 None -3 3 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assayInhibition of human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of 5-HT-induced increase in Ca2+ level pretreated for 10 mins by cAMP accumulation assay
ChEMBL 429 7 0 8 2.7 COc1ccc(S(=O)(=O)n2cc(/C=N/N=C/N(C)C)c3c([N+](=O)[O-])cccc32)cc1 10.1016/j.bmc.2015.01.032
71769066 91527 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
CHEMBL2414712 91527 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hrAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced cAMP accumulation pretreated for 10 mins before 5HT addition measured after 1 hr
ChEMBL 536 6 0 7 5.1 COc1cc(C)c(Cl)cc1S(=O)(=O)n1c(-c2ccccc2)c(/C=N/N2CCN(C)CC2)c2ccccc21 10.1016/j.bmc.2013.05.051
54585848 62405 6 None -5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783971 62405 6 None -5 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 316 3 0 4 3.1 CN1CCc2c(c3cc(C#N)ccc3n2CCc2ccccn2)C1 10.1016/j.bmcl.2009.04.128
20901142 10663 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1171500 10663 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 401 4 1 8 3.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
24763352 62294 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783601 62294 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulationAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
46880759 6055 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080899 6055 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
53319628 57357 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668583 57357 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 nan
44403089 133106 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL371469 133106 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
24783294 176138 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
CHEMBL459987 176138 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
71814155 91162 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
CHEMBL2407551 91162 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 minsAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins
ChEMBL 425 4 3 5 2.1 O=C1c2[nH]nc(NS(=O)(=O)c3cccc4ccccc34)c2CCN1C1CCNCC1 10.1016/j.bmcl.2013.05.100
20901136 10867 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1173365 10867 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 439 5 1 9 4.0 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2ccco2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
45113530 14108 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095274 14108 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199079 14108 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
46189982 129243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675194 129243 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 373 6 2 7 2.1 CNc1nn2c(C)c(CCCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
18591267 10539 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170282 10539 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 485 6 1 9 4.4 COc1ccccc1CNc1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
49799656 10872 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173432 10872 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL3216262 10872 3 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 450 6 0 9 2.8 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
57391567 71193 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71193 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71193 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
18560184 10761 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1172398 10761 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCCC2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
86302554 110344 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110344 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assayAntagonist activity at human 5-HT6 receptor assessed as inhibition of 5-HT-induced cAMP level treated for 10 mins prior to 5-HT challenge for 30 mins by homogeneous time-resolved fluorescent assay
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
44433199 88348 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236314 88348 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24771120 183518 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 183518 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formationAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
9978683 18487 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18487 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
16118923 59830 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 59830 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 59830 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
44403093 71094 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196094 71094 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
9950255 195140 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565723 195140 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIAAntagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
57398803 69399 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69399 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69399 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
44388956 62757 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178870 62757 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
10383646 18575 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18575 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
44389003 123318 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362487 123318 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46880709 7366 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
CHEMBL1086720 7366 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
20901169 10586 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
CHEMBL1170687 10586 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 4 1 8 5.2 Cc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(Cl)cc4)nnn3c3ccsc23)c1C 10.1016/j.bmc.2010.05.051
11723168 205761 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL94422 205761 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
44397689 71096 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196102 71096 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL373107 71096 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
46880758 6018 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080729 6018 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
16019343 10480 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1169894 10480 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NC2CCCCC2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
20901124 10531 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170271 10531 5 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 475 4 1 8 4.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(Nc1cccc(C(F)(F)F)c1)c1sccc12 10.1016/j.bmc.2010.05.051
18591266 10826 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173004 10826 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 6 1 8 4.5 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCCc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
45487140 197155 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583677 197155 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonistic activity at human HT6 receptor expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
54582938 62390 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783955 62390 6 None -1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 321 4 0 4 3.3 COc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
58357860 128505 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670281 128505 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
45113403 8980 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1098894 8980 1 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 344 2 1 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
9842551 126702 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365774 126702 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44126329 62389 6 None 2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783954 62389 6 None 2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 305 3 0 3 3.6 Cc1ccc2c(c1)c1c(n2CCc2ccccn2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18560255 10615 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170897 10615 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 465 5 1 9 4.5 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C)c(C)c4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
18559286 10888 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173575 10888 9 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 429 6 1 8 4.2 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCCC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
7183407 10889 12 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173576 10889 12 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 417 6 1 9 2.8 COCCNc1nc2c(S(=O)(=O)c3cc(C)ccc3C)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
162647425 178997 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4741978 178997 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
16116896 59824 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642861 59824 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739644 59824 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
53320746 59834 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642854 59834 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739685 59834 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
46224879 199862 3 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 199862 3 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
49799629 10834 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173062 10834 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 416 6 0 9 2.2 CN(C)CCN(C)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118512807 149859 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
CHEMBL3953555 149859 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assayAntagonist activity at human 5-HT6R expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP levels pre-treated for 10 mins before 30 mins stimulation with 5-HT by D2-dye based HTRF assay
ChEMBL 425 7 1 4 4.8 CC(C)Cc1cc(CNS(=O)(=O)c2ccc(C(C)(C)C)cc2)nn1-c1ccccc1 10.1016/j.bmcl.2017.07.031
16116899 59784 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642846 59784 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739232 59784 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
25123011 199508 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 199508 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIAAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as intracellular cAMP formation by RIA
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
11723168 205761 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL94422 205761 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
197033 197473 58 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
CHEMBL589390 197473 58 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.04.128
18559285 10823 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172939 10823 7 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 443 5 1 9 3.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NCC2CCCO2)c2sccc23)c1 10.1016/j.bmc.2010.05.051
197033 197473 58 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 197473 58 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assayAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production by LANCE assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
54579957 62399 4 None -36 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
CHEMBL1783964 62399 4 None -36 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE techniqueAntagonist activity at human recombinant 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular cAMP accumulation by LANCE technique
ChEMBL 291 3 0 3 3.3 CN1CCc2c(c3ccccc3n2CCc2ccncc2)C1 10.1016/j.bmcl.2009.04.128
56849578 68531 3 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922618 68531 3 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189935 68546 2 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68546 2 None - 1 Human 8.1 pIC50 = 8.1 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
44389099 64506 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182000 64506 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44389015 121816 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359876 121816 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44435538 90175 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
CHEMBL238770 90175 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP productionAntagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
44388943 62960 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL179277 62960 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptorInhibitory concentration against 5-HT stimulated cAMP production in HeLa cells stably transfected with human 5-HT6 receptor
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
53327611 69411 0 None 154 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None 154 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assayAntagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
53323436 59816 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642870 59816 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739585 59816 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16019366 10575 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
CHEMBL1170671 10575 4 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 455 5 1 9 4.5 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCc2cccs2)c2sccc23)cc1C 10.1016/j.bmc.2010.05.051
18559353 10540 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1170288 10540 11 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 479 6 1 9 5.0 COc1cccc(Nc2nc3c(S(=O)(=O)c4ccc(C(C)C)cc4)nnn3c3ccsc23)c1 10.1016/j.bmc.2010.05.051
53326022 59825 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642863 59825 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739645 59825 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44435618 88354 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236334 88354 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46224881 199278 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL601902 199278 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 316 2 0 2 4.9 Cc1ccc(/C=C\n2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
53323600 57353 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668579 57353 2 None - 1 Human 6.0 pIC50 = 6.0 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
20901270 10556 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170465 10556 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 441 4 1 8 4.6 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(Nc1ccccc1)c1sccc12 10.1016/j.bmc.2010.05.051
16019292 10891 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10891 7 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53319443 59838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642858 59838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739696 59838 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
16956204 10878 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173501 10878 5 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 529 6 1 9 4.6 COc1ccccc1CNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16117154 59831 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642881 59831 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739657 59831 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
46880658 6303 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1082199 6303 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassayAntagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced intracellular cAMP level after 10 mins by radioimmunoassay
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
16118797 59781 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642852 59781 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739216 59781 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formationAntagonist activity at cloned human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5HT-induced cyclic AMP formation
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
44435620 148462 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394231 148462 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassayAntagonist activity at human 5HT6 expressed in HeLa cells assessed as intracellular cAMP level by radioimmunoassay
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44474629 13965 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL1197581 13965 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL577570 13965 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assayAntagonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as inhibition of 5-HT-stimulated cAMP production after 30 mins by HTRF assay
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
57393365 71206 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP productionAntagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
23624309 176159 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460195 176159 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassayAntagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells assessed as blockage of 5-HT-stimulated cAMP formation after 10 mins by radioimmunoassay
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
44403092 70290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL195018 70290 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10272325 71397 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL196619 71397 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of cAMP production in HeLa cells expressing human 5-HT6 receptorInhibition of cAMP production in HeLa cells expressing human 5-HT6 receptor
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
16019394 10764 8 None 37 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172405 10764 8 None 37 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 447 4 1 8 4.6 O=S(=O)(c1ccc(Cl)cc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
16019604 10871 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
CHEMBL1173431 10871 3 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP productionAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production
ChEMBL 449 6 1 8 4.1 Cc1ccc(S(=O)(=O)c2nnn3c2nc(NCCc2ccccc2)c2sccc23)cc1 10.1016/j.bmc.2010.05.051
3241 3465 17 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918649 3465 17 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
CHEMBL1210710 3465 17 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assayAntagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
11256720 2024 73 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
9444 2024 73 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
CHEMBL1083390 2024 73 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
DB12680 2024 73 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assayInverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2020.112765
44126272 197471 4 None -14 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589388 197471 4 None -14 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 358 3 0 2 4.9 CN1CCc2c(c3cc(C(F)(F)F)ccc3n2CCc2ccccc2)C1 10.1016/j.bmcl.2009.11.037
44126326 197938 6 None -32 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592753 197938 6 None -32 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE methodAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
ChEMBL 322 3 0 2 4.3 Cc1ccc2c(c1)c1c(n2CCc2ccc(F)cc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
46884709 7997 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091208 7997 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 minsAntagonist activity at human 5HT6 receptor in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation pretreated for 15 mins before serotonin challenge measured after 30 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
58357740 128509 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3670285 128509 0 None - 1 Human 6.0 pIC50 = 6 Functional
Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.Functional Assay: Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP, were used. The level of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity.
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
58158749 138466 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785512 138466 0 None - 0 Human 10.3 pKd = 10.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
54752954 138421 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785100 138421 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
46189932 68543 3 None - 1 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68543 3 None - 1 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56655504 68527 2 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68527 2 None - 1 Human 9.3 pKd = 9.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44216882 138585 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786752 138585 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
58158721 138463 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785453 138463 0 None - 0 Human 9.0 pKd = 9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595671 65347 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834333 65347 0 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
6918542 203216 20 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 203216 20 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptorAntagonistic activity towards 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44240860 138652 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787525 138652 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593934 65364 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65364 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
56595402 65306 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595531 65315 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
CHEMBL1834235 65315 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
56593797 65356 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834341 65356 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
56593933 65363 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
CHEMBL1834349 65363 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
58158719 138462 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785431 138462 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
59339383 138606 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787014 138606 0 None - 0 Human 8.0 pKd = 8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595670 65346 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834332 65346 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
56593643 65349 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834335 65349 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56593803 65360 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
CHEMBL1834346 65360 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
58158748 138563 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786563 138563 0 None - 0 Human 7.0 pKd = 7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
10356663 111451 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111451 0 None - 1 Human 7.0 pKd = 7 Functional
Antagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assayAntagonistic activity towards 5-hydroxytryptamine 6 receptor was evaluated in cAMP assay
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
56595667 65320 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834241 65320 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158707 138519 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786087 138519 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595533 65316 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
CHEMBL1834237 65316 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
56593799 65358 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834343 65358 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127033666 138442 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785278 138442 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595280 65305 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834225 65305 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
25056080 65359 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65359 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
56595280 65305 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834225 65305 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
25056080 65359 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834345 65359 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593644 65350 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834336 65350 0 None - 0 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
127031618 138639 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
CHEMBL3787388 138639 0 None - 0 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 405 4 2 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(N)cc1 10.1016/j.bmcl.2016.02.001
56595529 65314 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
CHEMBL1834234 65314 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
56595529 65314 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
CHEMBL1834234 65314 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
56593646 65352 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834338 65352 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
58158738 138433 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785231 138433 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
56593642 65348 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834334 65348 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158668 138499 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785864 138499 0 None - 0 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593798 65357 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834342 65357 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
58158739 138627 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787201 138627 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56593932 65362 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
CHEMBL1834348 65362 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
59339335 138477 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785626 138477 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
53310757 138604 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786973 138604 0 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56849719 68540 2 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68540 2 None - 0 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationAntagonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56595402 65306 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595668 65321 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834242 65321 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595405 65309 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
70878688 65309 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
CHEMBL1834229 65309 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
56595535 65318 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
CHEMBL1834239 65318 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
56595402 65306 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595402 65306 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834226 65306 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
44240753 138580 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786693 138580 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
44240802 138651 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787508 138651 0 None - 0 Human 8.3 pKd = 8.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595403 65307 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834227 65307 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
24855787 65303 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834221 65303 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
56595404 65308 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
CHEMBL1834228 65308 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
56595666 65319 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834240 65319 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
56593931 65361 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
CHEMBL1834347 65361 0 None - 0 Human 8.2 pKd = 8.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
56593936 65366 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834352 65366 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
56593936 65366 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834352 65366 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
127032424 138581 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786703 138581 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595406 65311 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
CHEMBL1834230 65311 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
56595534 65317 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
CHEMBL1834238 65317 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
56593645 65351 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834337 65351 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
56593647 65353 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834339 65353 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
56665086 65355 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834340 65355 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
58158682 138438 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785259 138438 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595407 65312 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
CHEMBL1834231 65312 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
56595669 65322 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834243 65322 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
58158709 138629 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787246 138629 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assayAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO cells assessed as inhibition of agonist induced intracellular calcium levels by aequorin assay
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595408 65313 0 None - 0 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
CHEMBL1834232 65313 0 None - 0 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescenceAntagonist activity at human recombinant 5-HT6 receptor expressed in CHO aequoscreen recombinant cell line assessed as inhibition of alpha-methylserotonin-induced luminescence
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
56849576 68529 3 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68529 3 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849576 68529 3 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922616 68529 3 None - 0 Human 9.9 pKi = 9.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
10131620 102005 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413990 102005 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040186 102005 1 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 331 4 2 5 2.0 CNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44156626 57364 3 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668590 57364 3 None - 1 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 350 3 1 6 2.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
56655571 68545 30 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922632 68545 30 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 4 1 7 2.3 CNc1nn2c(C)c(N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849575 68528 3 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922615 68528 3 None - 0 Human 9.7 pKi = 9.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 351 3 2 7 2.1 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326176 57360 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668586 57360 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44516817 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668584 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156754 6432 3 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6432 3 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
44516817 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44516817 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44516817 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1668584 57358 4 None 1023 2 Human 9.6 pKi = 9.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918032 57338 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668564 57338 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(C)cc(COC)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
53322258 57339 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668565 57339 3 None - 1 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56655504 68527 2 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922614 68527 2 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3453 13 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3453 13 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3453 13 None - 1 Mouse 9.5 pKi = 9.5 Functional
Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
56849579 68532 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922619 68532 3 None - 1 Human 9.5 pKi = 9.5 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 1 7 2.0 CNc1nn2c(N(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44156628 6636 3 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6636 3 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44156622 57366 3 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668592 57366 3 None - 1 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
44156752 6502 3 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6502 3 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
46190037 68551 2 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922638 68551 2 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 407 5 1 7 2.9 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53326177 57362 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668588 57362 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44156624 57365 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668591 57365 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 334 3 1 6 2.4 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
46189932 68543 3 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922630 68543 3 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46867519 6430 3 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6430 3 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
46189984 68548 1 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922635 68548 1 None - 1 Human 9.3 pKi = 9.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
53316984 57342 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668568 57342 3 None - 1 Human 9.3 pKi = 9.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(CO)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849578 68531 3 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922618 68531 3 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 2.0 CNc1nn2c(NC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53326178 57370 3 None - 1 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668596 57370 3 None - 1 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 368 3 1 6 3.0 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
46189935 68546 2 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922633 68546 2 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
46190034 68549 0 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922636 68549 0 None - 1 Human 9.2 pKi = 9.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 5 1 7 2.3 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3453 13 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3453 13 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3453 13 None - 1 Mouse 9.1 pKi = 9.1 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
44155994 57345 3 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668571 57345 3 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
6918479 56367 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
CHEMBL1642114 56367 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm201079g
56849857 68550 2 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922637 68550 2 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 391 5 1 7 2.4 CNc1nn2c(C)c(CN(C)C)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
56655505 68542 2 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922629 68542 2 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(C)cc(CN)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44155992 57346 3 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668572 57346 3 None - 1 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1016/j.bmc.2010.12.055
53322935 57363 3 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668589 57363 3 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
44155874 57315 15 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668500 57315 15 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
44155874 57315 15 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668500 57315 15 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579181 190358 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
CHEMBL518591 190358 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 374 2 0 4 3.6 CN1CCc2cc3ccn(S(=O)(=O)c4cccc(Cl)c4)c3cc2CC1 10.1016/j.bmcl.2008.08.010
46890885 6823 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1084315 6823 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46189980 68552 2 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922639 68552 2 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
6918629 68576 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922716 68576 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
46189987 68547 2 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
CHEMBL1922634 68547 2 None - 1 Human 8.9 pKi = 8.9 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 363 4 2 7 1.8 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(F)c1 10.1021/jm201079g
53324896 57359 3 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668585 57359 3 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 302 3 1 6 1.9 CNc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110702 170711 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL446054 170711 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579085 189846 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517828 189846 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9944808 101997 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413989 101997 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040139 101997 5 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 317 3 2 5 1.5 Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476436 81935 5 None 7413 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 81935 5 None 7413 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
56849717 68539 2 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922626 68539 2 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 359 5 1 7 2.0 CNc1nn2c(CN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849716 68538 1 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922625 68538 1 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 331 4 2 7 1.4 CNc1nn2c(CN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476434 81934 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172185 81934 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 10.1016/j.bmcl.2012.05.036
44155875 60658 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1762568 60658 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
10286330 182218 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
CHEMBL479067 182218 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptorAntagonist activity at 5HT6 receptor
ChEMBL 302 3 2 3 2.2 O=S(=O)(Nc1ccc2c(c1)CCNCC2)c1ccccc1 10.1016/j.bmcl.2008.08.010
44579131 181042 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
CHEMBL477386 181042 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2ccc3cc4c(cc32)CCNCC4)c1 10.1016/j.bmcl.2008.08.010
44579182 182059 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478871 182059 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 340 2 1 4 2.7 Cn1cc(S(=O)(=O)c2ccccc2)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53320929 57368 3 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668594 57368 3 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 332 3 2 7 1.9 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
5113605 79313 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL211577 79313 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1016/j.bmc.2013.05.040
44579132 181043 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477387 181043 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 327 2 1 5 2.0 O=S(=O)(c1ccccn1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46891114 6547 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1083298 6547 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 5 0 5 3.2 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
46891174 6806 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
CHEMBL1084214 6806 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 485 5 0 5 3.5 COc1cc(C)c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c(C)c1C 10.1016/j.bmcl.2010.04.085
53323601 57367 3 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668593 57367 3 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
56849713 68535 2 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68535 2 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849713 68535 2 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922622 68535 2 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 8 2 8 2.3 CNc1nn2c(NCCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
3232 3453 13 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3453 13 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3453 13 None - 1 Mouse 6.9 pKi = 6.9 Functional
Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
53318300 57314 0 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668499 57314 0 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 305 3 0 6 2.3 CSc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44476804 81938 2 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172190 81938 2 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 392 3 0 7 2.4 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccc(F)cc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
9822810 69159 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69159 0 None - 0 Rat 7.9 pKi = 7.9 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of rat striatumBinding affinity against 5-hydroxytryptamine 6 receptor of rat striatum
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
46882521 5635 0 None - 2 Human 6.9 pKi = 6.9 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5635 0 None - 2 Human 6.9 pKi = 6.9 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
46891053 6433 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082764 6433 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 7 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4nsnc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891175 6865 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084482 6865 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
53323599 57349 3 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668575 57349 3 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 323 3 0 6 2.4 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
52915983 60664 3 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762574 60664 3 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 371 3 1 7 1.6 Cc1cc(C)n2nc(N3CCNCC3)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
44476607 81940 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172192 81940 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
44156502 60659 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762569 60659 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 330 3 0 6 2.2 Cc1cc(C)n2nc(N(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
58149665 81932 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172183 81932 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
45488151 195235 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
CHEMBL566213 195235 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
53320927 57344 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668570 57344 3 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 339 3 0 6 2.9 CSc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmc.2010.12.055
46882583 5679 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
CHEMBL1078491 5679 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 453 5 2 6 2.6 CN1CCOc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc21 10.1016/j.bmcl.2009.09.027
68014793 91496 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413987 91496 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 323 4 1 3 4.2 CNc1cc(-c2ccccc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
53324895 57340 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
CHEMBL1668566 57340 3 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)nc2c(S(=O)(=O)c3ccccc3)c(SC)nn12 10.1016/j.bmc.2010.12.055
45102707 5680 0 None - 1 Human 6.8 pKi = 6.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
CHEMBL1078492 5680 0 None - 1 Human 6.8 pKi = 6.8 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 465 6 2 6 3.9 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2009.09.027
46890103 7070 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085361 7070 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 437 4 1 5 2.3 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(N)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
31386 96158 90 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL263327 96158 90 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 218 2 0 2 2.5 O=S(=O)(c1ccccc1)c1ccccc1 10.1016/j.bmc.2013.05.040
45488139 195272 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
CHEMBL566410 195272 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
45488143 196089 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
CHEMBL571762 196089 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
21254909 57316 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668501 57316 2 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
56849714 68536 4 None - 1 Human 7.8 pKi = 7.8 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922623 68536 4 None - 1 Human 7.8 pKi = 7.8 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488166 195237 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
CHEMBL566219 195237 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
46867655 6578 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
CHEMBL1083389 6578 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 411 3 1 7 2.2 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCCC2 10.1021/jm100350r
56849577 68530 3 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
CHEMBL1922617 68530 3 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 385 3 2 7 2.8 CNc1nn2c(N)c(Cl)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 10.1021/jm201079g
10934 1293 111 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
2955 1293 111 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
782 1293 111 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
CHEMBL1043 1293 111 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
DB00250 1293 111 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N 10.1016/j.bmc.2013.05.040
46890886 6824 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084316 6824 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 9 1 5 3.6 CCN(CC)CCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46891112 7190 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085965 7190 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 5 0 5 3.4 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46882522 5636 0 None - 2 Human 6.7 pKi = 6.7 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5636 0 None - 2 Human 6.7 pKi = 6.7 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46190041 68553 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922640 68553 0 None - 0 Human 8.7 pKi = 8.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 387 6 1 7 2.3 CNc1nn2c(C)c(CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
44476611 81939 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172191 81939 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 343 3 2 7 1.3 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCNC3 10.1016/j.bmcl.2012.05.036
52918030 57343 3 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668569 57343 3 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 4 1 7 2.1 CSc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
25110703 189128 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL515624 189128 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
9924293 68554 0 None - 1 Human 8.6 pKi = 8.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922641 68554 0 None - 1 Human 8.6 pKi = 8.6 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1021/jm201079g
54238415 91492 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413983 91492 0 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 261 3 0 3 2.6 CN(C)c1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
56849581 68534 0 None - 1 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922621 68534 0 None - 1 Human 7.7 pKi = 7.7 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 402 7 1 8 1.9 CNc1nn2c(N(C)CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53324933 57317 2 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668502 57317 2 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
52915982 60665 3 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762575 60665 3 None - 0 Human 5.7 pKi = 5.7 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 374 6 0 7 2.1 Cc1cc(C)n2nc(OCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
10658135 91494 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413985 91494 4 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 247 3 1 3 2.6 CNc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46891113 6546 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083297 6546 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891111 6725 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1083909 6725 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 481 4 0 4 3.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891004 7066 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085351 7066 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890058 7169 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085835 7169 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 479 5 1 5 3.4 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46867524 6505 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083078 6505 3 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 356 3 0 6 2.4 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N(C)C)nn2c2c1CCC2 10.1021/jm100350r
52915869 60666 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762576 60666 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 373 6 1 7 2.2 Cc1cc(C)n2nc(NCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
45488165 195236 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL566218 195236 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46867523 6504 3 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083077 6504 3 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 342 3 0 6 2.1 CN(C)c1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
44155871 60661 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762571 60661 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
52915984 60667 3 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762577 60667 3 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 349 3 0 6 1.9 Cc1cc(C)n2nc([S+](C)[O-])c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
56849719 68540 2 None - 0 Human 8.5 pKi = 8.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922627 68540 2 None - 0 Human 8.5 pKi = 8.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 345 5 2 7 1.4 CNc1nn2c(CCN)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53322259 57347 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668573 57347 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 10.1016/j.bmc.2010.12.055
53320926 57341 3 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
CHEMBL1668567 57341 3 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 5 0 7 2.7 COCc1cc(C)n2nc(SC)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.bmc.2010.12.055
53326175 57354 3 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668580 57354 3 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
53319628 57357 0 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668583 57357 0 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 288 3 1 6 1.6 CNc1nn2cccnc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579180 182058 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478870 182058 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 394 2 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
53325519 57350 3 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668576 57350 3 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 349 3 1 7 2.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(O)cc1 10.1016/j.bmc.2010.12.055
10132329 102003 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413988 102003 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040182 102003 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 345 4 1 5 2.0 CN(C)c1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
45488131 196904 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
CHEMBL578411 196904 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
46890949 6369 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082485 6369 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 463 4 0 4 3.7 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890056 6374 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082494 6374 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 505 5 1 5 3.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CC4CCC(C3)N4C)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890946 6520 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1083122 6520 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 509 8 1 6 3.0 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCN3CCOCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46891176 6866 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1084483 6866 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 489 5 0 4 4.2 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc(-c4ccccc4)c3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891005 7067 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085352 7067 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 457 4 0 5 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)C3=CC4CCOC4C=C3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891055 6435 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082766 6435 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 419 4 0 5 2.6 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891056 6436 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082767 6436 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 413 4 0 4 2.5 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891007 7069 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
CHEMBL1085354 7069 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 478 4 0 5 3.4 Cc1cnc2c(S(=O)(=O)N3CC(C(=O)N(C)C4CCN(C)CC4)c4ccccc43)cccc2c1 10.1016/j.bmcl.2010.04.085
56849720 68541 2 None - 0 Human 7.5 pKi = 7.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922628 68541 2 None - 0 Human 7.5 pKi = 7.5 Functional
Partial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationPartial agonist activity at human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 6 1 7 2.0 CNc1nn2c(CCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
45488152 197251 0 None - 0 Mouse 7.5 pKi = 7.5 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 197251 0 None - 0 Mouse 7.5 pKi = 7.5 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
53318267 57351 1 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668577 57351 1 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 10.1016/j.bmc.2010.12.055
53320928 57352 3 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668578 57352 3 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 376 4 0 7 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(N(C)C)cc1 10.1016/j.bmc.2010.12.055
44579183 182061 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478872 182061 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 342 2 1 3 2.5 O=S(=O)(c1ccccc1)N1CCCc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
56849715 68537 3 None - 1 Human 8.4 pKi = 8.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922624 68537 3 None - 1 Human 8.4 pKi = 8.4 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
56849856 68544 3 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922631 68544 3 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 373 4 2 7 2.2 CNc1nn2c(C)c(NC(C)=O)c(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
53323600 57353 2 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668579 57353 2 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 357 3 0 6 3.1 CSc1nn2cccnc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
68014784 91495 1 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413986 91495 1 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 324 4 1 4 3.6 CNc1cc(-c2cccnc2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
52915980 60662 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762572 60662 3 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 6 0 7 2.2 Cc1cc(C)n2nc(N(C)CCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
77956 72673 85 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2009408 72673 85 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 233 2 1 3 2.1 Nc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
44476801 81937 2 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172189 81937 2 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HE293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
45488152 197251 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 197251 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at human 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
45488152 197251 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 197251 0 None - 0 Mouse 8.3 pKi = 8.3 Functional
Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
46890948 6368 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1082484 6368 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 497 4 0 4 4.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3cccc4c(Cl)cccc34)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46891006 7068 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
CHEMBL1085353 7068 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 471 4 0 6 2.3 CN1CCC(N(C)C(=O)C2CN(S(=O)(=O)c3ccc4c(c3)OCCO4)c3ccccc32)CC1 10.1016/j.bmcl.2010.04.085
46890059 7170 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085836 7170 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 555 7 1 5 4.9 COc1ccc(S(=O)(=O)N2CC(C(=O)NC3CCN(Cc4ccccc4)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
3232 3453 13 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
3248571 3453 13 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
CHEMBL60264 3453 13 None - 1 Mouse 7.3 pKi = 7.3 Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assayAntagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm901672k
1472656 34405 22 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1429795 34405 22 None - 1 Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
460659 51131 9 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
CHEMBL1581846 51131 9 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 263 2 3 5 1.3 Nc1ccc(S(=O)(=O)c2ccc(N)c(N)c2)cc1 10.1016/j.bmc.2013.05.040
46882520 5779 0 None - 2 Human 8.2 pKi = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5779 0 None - 2 Human 8.2 pKi = 8.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
44155876 57348 3 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668574 57348 3 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2010.12.055
46891054 6434 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082765 6434 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 517 4 0 5 4.7 Cc1c(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.04.085
46890106 6901 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
CHEMBL1084614 6901 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 557 6 0 6 4.5 COc1cccc(N2CCN(C(=O)C3CN(S(=O)(=O)c4ccc(OC)c5ccccc45)c4ccccc43)CC2)c1 10.1016/j.bmcl.2010.04.085
45102708 5693 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078595 5693 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at 5HT6 receptorAgonist activity at 5HT6 receptor
ChEMBL 468 6 2 7 2.0 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(N2CCOCC2)nc1 10.1016/j.bmcl.2009.09.027
56849580 68533 4 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
CHEMBL1922620 68533 4 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulationInhibition of human recombinant 5-HT6 receptor expressed in human HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm201079g
52918031 57361 3 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
CHEMBL1668587 57361 3 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2010.12.055
44579130 181041 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL477385 181041 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579129 181555 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL478223 181555 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
44579133 189644 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
CHEMBL517503 189644 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assayAntagonist activity at 5HT6 receptor expressed in HeLa cells assessed as 5HT-induced cAMP accumulation by chemiluminescence assay
ChEMBL 332 2 1 5 2.6 O=S(=O)(c1ccsc1)n1ccc2cc3c(cc21)CCNCC3 10.1016/j.bmcl.2008.08.010
46890057 6449 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082818 6449 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 493 5 0 5 3.7 COc1ccc(S(=O)(=O)N2CC(C(=O)N(C)C3CCN(C)CC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890105 7118 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085608 7118 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 4 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CCNCC3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
53319627 57355 1 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
CHEMBL1668581 57355 1 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 371 3 0 6 3.4 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 10.1016/j.bmc.2010.12.055
9822810 69159 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69159 0 None - 0 Human 8.1 pKi = 8.1 Functional
Binding affinity against 5-hydroxytryptamine 6 receptor of human caudateBinding affinity against 5-hydroxytryptamine 6 receptor of human caudate
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
52915979 60663 4 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762573 60663 4 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 387 7 1 7 2.5 Cc1cc(C)n2nc(NCCCN(C)C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
46890947 6367 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1082483 6367 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 490 8 1 6 3.5 COc1ccc(S(=O)(=O)N2CC(C(=O)NCCCn3ccnc3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
46890887 6825 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
CHEMBL1084317 6825 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 495 10 1 5 4.0 CCN(CC)CCCNC(=O)C1CN(S(=O)(=O)c2ccc(OC)c3ccccc23)c2ccccc21 10.1016/j.bmcl.2010.04.085
46890104 7071 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
CHEMBL1085362 7071 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assayAntagonist activity at human 5HT6 expressed in CHO cells by FLIPR 384 assay
ChEMBL 451 5 1 5 2.6 COc1ccc(S(=O)(=O)N2CC(C(=O)N3CC(CN)C3)c3ccccc32)c2ccccc12 10.1016/j.bmcl.2010.04.085
9925009 102004 1 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413991 102004 1 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL3040183 102004 1 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 359 4 2 5 1.9 CC(=O)Nc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
640912 91493 7 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL2413984 91493 7 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
ChEMBL 248 3 0 3 2.5 COc1ccccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
46867654 6577 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
CHEMBL1083388 6577 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP releaseAntagonist activity at human 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP release
ChEMBL 397 3 1 7 1.8 Cc1nc2c(S(=O)(=O)c3ccccc3)c(N3CCNCC3)nn2c2c1CCC2 10.1021/jm100350r
52915868 60660 6 None - 1 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762570 60660 6 None - 1 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP production after 2 hrs
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
53319629 57369 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
CHEMBL1668595 57369 3 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrsAntagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs
ChEMBL 346 4 1 7 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 10.1016/j.bmc.2010.12.055
4223 3929 88 None -562 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3929 88 None -562 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3929 88 None -562 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3929 88 None -562 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3929 88 None -562 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
10131112 1523 21 None 14 8 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
8428 1523 21 None 14 8 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331
CHEMBL364005 1523 21 None 14 8 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 16055331




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9921064 126657 18 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 126657 18 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at 5-HT6 receptor (unknown origin)Agonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
10337743 4013 16 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
8429 4013 16 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
CHEMBL571858 4013 16 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assayAgonist activity at human 5-HT6 receptor expressed in HeLa cells after 10 mins by scintillation proximity assay
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
91971999 138302 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781299 138302 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 517 7 1 5 3.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
46189984 68548 1 None - 1 Human 9.6 pIC50 = 9.6 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1922635 68548 1 None - 1 Human 9.6 pIC50 = 9.6 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 379 4 2 7 2.3 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
118465011 138304 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781323 138304 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
56655504 68527 2 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922614 68527 2 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 317 3 2 7 1.5 CNc1nn2c(N)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465045 138239 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780579 138239 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 545 7 1 5 4.6 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
52918031 57361 3 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668587 57361 3 None - 1 Human 9.5 pIC50 = 9.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 346 5 1 7 2.1 CNc1nn2c(COC)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465023 138310 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781452 138310 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118464996 138188 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3779904 138188 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
46189935 68546 2 None - 1 Human 9.3 pIC50 = 9.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922633 68546 2 None - 1 Human 9.3 pIC50 = 9.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 4 2 7 1.7 CNc1nn2c(C)c(CN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189980 68552 2 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922639 68552 2 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 5 2 7 1.7 CNc1nn2c(C)c(CCN)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
46189932 68543 3 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922630 68543 3 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 331 3 2 7 1.8 CNc1nn2c(C)c(N)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
118465171 138216 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780274 138216 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(F)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
10383682 119883 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
CHEMBL353389 119883 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition against human 5-hydroxytryptamine 6 receptorInhibition against human 5-hydroxytryptamine 6 receptor
ChEMBL 356 5 1 1 5.1 CN(C)CCCc1c(-c2cccc(Br)c2)[nH]c2ccccc12 10.1021/jm0309452
53326176 57360 3 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668586 57360 3 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 302 3 1 6 1.9 CNc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
44476436 81935 5 None - 1 Human 9.1 pIC50 = 9.1 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172186 81935 5 None - 1 Human 9.1 pIC50 = 9.1 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
53326177 57362 3 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668588 57362 3 None - 1 Human 9.1 pIC50 = 9.1 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 332 4 2 7 1.4 CNc1nn2c(C)cc(CO)nc2c1S(=O)(=O)c1ccccc1 nan
118464995 138289 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781179 138289 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 439 7 1 5 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
44155109 8090 3 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8090 3 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44156863 7995 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 7995 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
118464998 138338 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781801 138338 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc2cccc(CCNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
118465054 138299 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781263 138299 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 8 2 6 3.5 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCNCC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
44155107 7996 3 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 7996 3 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
118465064 138194 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779974 138194 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 529 7 2 5 4.0 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(Br)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
68303363 129238 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
CHEMBL3675189 129238 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 430 7 1 8 3.1 CCOC(=O)Cc1c(C)nc2c(S(=O)(=O)c3ccccc3)c(NC(C)C)nn2c1C nan
118465035 138202 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780141 138202 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 453 7 2 5 3.5 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118464997 138295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781239 138295 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 457 7 1 5 3.3 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
10427672 104515 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113554 104515 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2ccc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
118465048 138196 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3780011 138196 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 497 8 1 6 3.9 COc1ccc2cccc(C(C)(C)CNS(=O)(=O)c3ccc(OC)c(N4CCN(C)CC4)c3)c2c1 10.1021/acsmedchemlett.5b00466
70245924 81941 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172193 81941 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
46830134 8133 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8133 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44476514 81936 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172187 81936 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
118465025 138308 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781399 138308 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2ccc(F)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
196129 67456 12 None 1 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67456 12 None 1 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
118465050 138266 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780861 138266 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 531 7 2 5 4.3 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
15619875 69117 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL193351 69117 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 1 1 1 3.8 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(C)CC1 10.1016/j.bmcl.2005.06.067
73354882 89263 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89263 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73347307 89268 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89268 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 66 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 66 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 66 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 66 None -169 54 Human 7.0 pIC50 = 7 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
44403367 70731 4 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL195239 70731 4 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.3 CC(C)c1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
73351904 89270 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376489 89270 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 270 3 2 2 3.6 Cc1[nH]c2ccc(OC(C)C)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
73353367 89274 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
CHEMBL2376493 89274 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 274 2 1 2 4.0 CCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
73351905 89272 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376491 89272 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
4189 205195 91 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
3198 203802 73 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
135398737 944 89 None -4 91 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -4 91 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -4 91 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -4 91 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -4 91 Human 8.0 pIC50 = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
118465024 138298 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781260 138298 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
118465038 138344 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781948 138344 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 471 7 2 5 3.7 COc1ccc(S(=O)(=O)NCC(C)(C)c2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
53322638 56381 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642128 56381 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)C(C)CC2=O 10.1016/j.bmcl.2010.12.007
10451504 104478 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
CHEMBL3113350 104478 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1Cl 10.1016/j.bmc.2014.01.003
20901117 10576 3 None - 1 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10576 3 None - 1 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
6761 67457 17 None -9 18 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67457 17 None -9 18 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44155876 57348 3 None - 1 Human 7.0 pIC50 = 7.0 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668574 57348 3 None - 1 Human 7.0 pIC50 = 7.0 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
4601 205020 29 None -2 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205020 29 None -2 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205020 29 None -2 17 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
1530 2151 44 None -58 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -58 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -58 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -58 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -58 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
49864601 15487 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222137 15487 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 4 0 2 5.0 CC(C)N(c1cccc(I)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
1588 2294 24 None -30 43 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2294 24 None -30 43 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2294 24 None -30 43 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2294 24 None -30 43 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2294 24 None -30 43 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
11724112 104488 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113360 104488 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 329 4 1 6 2.0 CCOc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
9979748 104522 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113561 104522 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(C)cc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
10472756 104483 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
CHEMBL3113355 104483 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 0 6 2.4 C/N=c1/c(S(=O)(=O)c2ccccc2)c(SC)nc2ccccn12 10.1016/j.bmc.2014.01.003
5 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
2812 4711 96 None -36 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -36 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
11743064 35724 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL144265 35724 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
448537 159703 86 None -35 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -35 25 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
53319229 56277 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
CHEMBL1641610 56277 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 3 0 5 2.5 Cc1ccc(S(=O)(=O)N2CCC(=O)c3c(N4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2010.12.007
44476704 81931 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172182 81931 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
135398745 2869 108 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -4 65 Human 7.9 pIC50 = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
18180076 15426 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221497 15426 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 4 1 4 3.4 CN1CCN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
5 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 66 None -169 54 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
2600 3720 73 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3720 73 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3720 73 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3720 73 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3720 73 None -5 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5323 201101 99 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
CHEMBL62193 201101 99 None - 1 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
11236269 128783 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
CHEMBL367088 128783 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
11113605 10407 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 10407 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
54576142 66162 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852341 66162 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216098 66162 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 485 7 1 5 4.7 Cc1nc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
180 397 50 None -99 38 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -99 38 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -99 38 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -99 38 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -99 38 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
156018181 177233 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
CHEMBL4643549 177233 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 430 5 1 6 4.0 CC(C)c1ccc(S(=O)(=O)Nc2ccc3nc(N4CCN(C)CC4)sc3c2)cc1 10.1016/j.ejmech.2018.11.017
4211 57517 81 None 1 4 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57517 81 None 1 4 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
45109862 7353 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 7353 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
52915868 60660 6 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762570 60660 6 None - 1 Human 6.8 pIC50 = 6.8 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
73453 29403 22 None -10 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29403 22 None -10 17 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
53318694 56380 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642127 56380 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 3 0 5 4.1 Cc1ccc2c(c1N1CCN(C)CC1)C(=O)CC(C)N2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
68262106 129239 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675190 129239 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 401 5 1 7 1.9 CNc1nn2c(C)c(CC(=O)N(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
2585 790 100 None -109 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 790 100 None -109 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 790 100 None -109 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 790 100 None -109 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 790 100 None -109 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1548953 205945 24 None -3 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205945 24 None -3 17 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
11071079 110104 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 110104 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
134551 355 25 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -6 21 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
118465034 138215 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780270 138215 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
46866711 15494 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
CHEMBL1222234 15494 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2010.06.150
169713 79751 17 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
CHEMBL21343 79751 17 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 309 3 2 2 2.6 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2NC1 10.1016/j.bmcl.2009.09.002
6918647 100278 2 None 50 14 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
CHEMBL292759 100278 2 None 50 14 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
58149663 126900 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659969 126900 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
3117 206106 100 None -5 16 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -5 16 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
134 2478 19 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2478 19 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2478 19 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2478 19 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2478 19 None -63 67 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
53321318 56374 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642121 56374 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 6 3.4 COc1cc2c(cc1N1CCN(C)CC1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
1209 1628 69 None -12 31 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1628 69 None -12 31 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1628 69 None -12 31 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1628 69 None -12 31 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1628 69 None -12 31 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
124 2933 44 None -100 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2933 44 None -100 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2933 44 None -100 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2933 44 None -100 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2933 44 None -100 32 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
54577891 66242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 66242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 66242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of 5HT6 receptor by competition binding assayInhibition of 5HT6 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
102 4064 44 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4064 44 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4064 44 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4064 44 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4064 44 None -173 49 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
53323972 56373 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642120 56373 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
135398737 944 89 None -4 91 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
38 944 89 None -4 91 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
722 944 89 None -4 91 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
CHEMBL42 944 89 None -4 91 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
DB00363 944 89 None -4 91 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2014.01.003
46884709 7997 3 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 7997 3 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
20901115 10862 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10862 5 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
126720440 162476 0 None 72 5 Human 7.8 pIC50 = 7.8 Binding
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4175829 162476 0 None 72 5 Human 7.8 pIC50 = 7.8 Binding
Partial inverse agonist activity at 5HT6R (unknown origin)Partial inverse agonist activity at 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
71695200 129240 5 None - 0 Human 6.8 pIC50 = 6.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675191 129240 5 None - 0 Human 6.8 pIC50 = 6.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 472 9 1 8 2.2 CNc1nn2c(C)c(CCC(=O)N(C)CCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
3397 203777 104 None -1 2 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 203777 104 None -1 2 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
53323601 57367 3 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL1668593 57367 3 None - 1 Human 7.8 pIC50 = 7.8 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 306 3 1 6 1.7 CNc1nn2cccnc2c1S(=O)(=O)c1ccc(F)cc1 nan
11741686 104479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
CHEMBL3113351 104479 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 399 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2014.01.003
5 139 66 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 66 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 66 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 66 None -169 54 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
25070582 61125 21 None - 1 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
CHEMBL1770373 61125 21 None - 1 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to 5-HT6 receptorBinding affinity to 5-HT6 receptor
ChEMBL 239 2 1 3 1.8 c1ccc(Cc2ncc3c(n2)CCNCC3)cc1 10.1016/j.bmcl.2010.11.120
6075 149575 36 None -13 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149575 36 None -13 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
2291 3135 52 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3135 52 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3135 52 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3135 52 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3135 52 None -12 12 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
7185124 10851 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173210 10851 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
45278882 7371 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 7371 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
176 394 63 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -5 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
42635204 187176 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495678 187176 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.3 O=S(=O)(NCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
10826203 161296 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
CHEMBL414668 161296 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 2 1 4.2 C1=C(c2c(-c3ccccc3)[nH]c3ccccc23)CCNC1 10.1016/j.bmcl.2005.06.067
118465009 138348 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3782008 138348 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 465 7 1 5 3.6 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
73356447 89276 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
CHEMBL2376561 89276 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 386 3 1 4 4.2 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2013.03.006
11724023 104490 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113362 104490 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 328 4 2 6 2.1 CCNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
276 3457 45 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
5312149 3457 45 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
CHEMBL431298 3457 45 None 81 13 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
1043 1552 13 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1552 13 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1552 13 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1552 13 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1552 13 None -23 28 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
118465087 138191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3779933 138191 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 503 7 2 5 3.5 COc1ccc(S(=O)(=O)NCCc2cccc3ccc(Br)cc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
118465051 138351 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3782049 138351 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 495 8 1 6 3.6 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCN(C)CC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
118465065 138321 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781574 138321 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 7 2 5 3.4 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccc(F)cc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
4106 2466 16 None -1 33 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
5358812 2466 16 None -1 33 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
89 2466 16 None -1 33 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
CHEMBL93240 2466 16 None -1 33 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm901674f
10470893 104489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113361 104489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 314 3 2 6 1.7 CNc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
150 2473 18 None -2 15 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2473 18 None -2 15 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2473 18 None -2 15 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2473 18 None -2 15 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2473 18 None -2 15 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
118465026 138272 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780950 138272 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 469 8 1 6 3.1 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
9924293 68554 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL1922641 68554 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 345 5 2 5 2.4 CCNc1cc(N2CCNCC2)ccc1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2013.05.040
118456745 138221 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780359 138221 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 425 7 2 5 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
73350387 89267 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL2376486 89267 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 258 2 2 2 3.6 CSc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
11333554 96213 19 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
CHEMBL26379 96213 19 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1016/j.ejmech.2013.03.006
44155994 57345 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668571 57345 3 None - 1 Human 7.7 pIC50 = 7.7 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(Cl)c1 nan
3245407 47841 23 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 47841 23 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 66 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 66 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 66 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 66 None -169 54 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
22504458 104487 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113359 104487 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 315 3 1 6 1.7 COc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72197486 102030 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393245 102030 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040361 102030 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 364 4 2 4 4.2 Clc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
124087 1362 106 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1362 106 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1362 106 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1362 106 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1362 106 None -28 15 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
49864530 15480 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222028 15480 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccccc1N1CCN(C)CC1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
3191 102385 93 None -15 25 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -15 25 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
31101 720 39 None -23 35 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 720 39 None -23 35 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 720 39 None -23 35 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 720 39 None -23 35 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 720 39 None -23 35 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10427896 104477 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113349 104477 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmc.2014.01.003
72197485 102016 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393244 102016 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040288 102016 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 348 4 2 4 3.6 Fc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
49799703 10890 3 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173577 10890 3 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
10885636 110527 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 110527 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44395664 66427 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
CHEMBL185850 66427 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
58149664 126901 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
CHEMBL3659970 126901 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
53322259 57347 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1668573 57347 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 367 3 0 6 3.6 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(Cl)cc1 nan
9931929 63133 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
CHEMBL179814 63133 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
2286 3134 48 None -26 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -26 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -26 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -26 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -26 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
2801 161325 56 None -5 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -5 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -5 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
44155992 57346 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
CHEMBL1668572 57346 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 351 3 0 6 3.0 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1cccc(F)c1 nan
11725253 104486 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113358 104486 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 347 3 1 6 1.4 C[S+]([O-])c1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
72548703 161019 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
53320009 56369 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 56369 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
274 3287 39 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5312145 3287 39 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
CHEMBL433461 3287 39 None -1 3 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm034142q
5 139 66 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 66 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 66 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 66 None -169 54 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human 5HT6 receptorInhibition of human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
42388639 187471 0 None - 6 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
CHEMBL497749 187471 0 None - 6 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 8 1 5 3.3 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmc.2008.04.023
2274 3124 53 None -23 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -23 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -23 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -23 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -23 32 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
1016 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -38 35 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
11743064 35724 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL144265 35724 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 423 3 1 6 3.4 CSc1nc2c(Br)cc(C)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
49864599 15485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccc(N2CCN(C)CC2)cc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222135 15485 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1ccc(N2CCN(C)CC2)cc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
5 139 66 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
5202 139 66 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
CHEMBL39 139 66 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
DB08839 139 66 None -169 54 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm901674f
2284 3133 27 None -12 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -12 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -12 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -12 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -12 28 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
1201549 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -77 20 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
133 2460 48 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2460 48 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2460 48 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2460 48 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2460 48 None -91 42 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
51003550 56371 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642118 56371 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
9998950 104493 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccc(Cl)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113365 104493 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 365 3 1 6 3.0 CSc1nc2ccc(Cl)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
10247229 120533 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL356781 120533 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019508 10811 6 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1172794 10811 6 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 401 4 1 8 3.6 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(NC(C)C)c2sccc23)c1 10.1016/j.bmc.2010.05.051
90644511 111174 13 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
CHEMBL3286556 111174 13 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 282 3 2 4 2.4 CNc1nc(Cc2ccccc2)nc2c1CCNC[C@@H]2C 10.1021/jm5003292
277 1274 55 None -93 45 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -93 45 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -93 45 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -93 45 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -93 45 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
42635027 186814 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL493625 186814 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 457 8 1 5 3.2 COc1ccc(S(=O)(=O)NCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
2162 41273 97 None -2 6 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41273 97 None -2 6 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
73356442 89266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376485 89266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 367 4 3 3 3.7 Cc1[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
68303508 129241 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675192 129241 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 486 10 1 8 2.6 CNc1nn2c(C)c(CCC(=O)N(C)CCCN(C)C)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
49864292 15419 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221452 15419 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 6 0 4 5.0 CN1CCN(c2cccc(N(Cc3ccccc3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
46934428 15484 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222134 15484 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 5 0 4 4.2 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
49864724 15516 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222364 15516 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 5 0 4 3.8 CCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
118465015 138212 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 7 1 5 3.7 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780252 138212 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 483 7 1 5 3.7 COc1ccc(S(=O)(=O)NCC2(c3cccc4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/acsmedchemlett.5b00466
6918689 85557 3 None 812 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
CHEMBL23038 85557 3 None 812 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
10531 1392 18 None -9 24 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1392 18 None -9 24 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1392 18 None -9 24 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1392 18 None -9 24 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1392 18 None -9 24 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1042 1551 20 None -5 16 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1551 20 None -5 16 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1551 20 None -5 16 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1551 20 None -5 16 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1551 20 None -5 16 Human 8.5 pIC50 = 8.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
10020454 104520 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2c(C)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113559 104520 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2c(C)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019576 10796 6 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10796 6 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
118465055 138253 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 451 7 2 5 3.3 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780744 138253 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 451 7 2 5 3.3 COc1ccc(S(=O)(=O)NCC2(c3cccc4ccccc34)CC2)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
44403358 70218 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 2 2 1 3.8 CCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194843 70218 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 260 2 2 1 3.8 CCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
44403375 70976 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 1 1 4.2 CCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL195759 70976 4 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 2 1 1 4.2 CCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
73347306 89264 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89264 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44155874 57315 15 None - 1 Human 7.5 pIC50 = 7.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57315 15 None - 1 Human 7.5 pIC50 = 7.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
72197668 102022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL2393246 102022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
CHEMBL3040325 102022 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 360 5 2 5 3.5 COc1cccc(Nc2nc(Cc3ccccc3)nc3c2CCNCC3)c1 10.1016/j.ejmech.2013.02.020
44403334 69967 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 258 3 2 2 3.2 CCc1[nH]c2ccc(OC)cc2c1C1CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194412 69967 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 258 3 2 2 3.2 CCc1[nH]c2ccc(OC)cc2c1C1CCNCC1 10.1016/j.bmcl.2005.06.067
4223 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 3929 88 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat hydroxytryptamine 6 receptorInhibition of rat hydroxytryptamine 6 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
68261572 129242 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3675193 129242 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 470 6 1 8 1.9 CNc1nn2c(C)c(CCC(=O)N3CCN(C)CC3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
3042 1386 31 None -51 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1386 31 None -51 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1386 31 None -51 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1386 31 None -51 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1386 31 None -51 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
165193 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3138 60 None -158 42 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4098 32289 24 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32289 24 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32289 24 None -22 11 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
118464990 138339 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781820 138339 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2cccc3c(OC)cccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
56849714 68536 4 None - 1 Human 7.5 pIC50 = 7.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922623 68536 4 None - 1 Human 7.5 pIC50 = 7.5 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 387 4 1 8 1.7 CNc1nn2c(N3CCOCC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
49799667 10812 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10812 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
53326548 56368 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642115 56368 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
3158 55974 21 None -851 20 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -851 20 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
59636980 125316 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 377 5 0 7 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 nan
CHEMBL3648343 125316 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 377 5 0 7 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(OC)cc1 nan
2247 502 77 None -53 41 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -53 41 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -53 41 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -53 41 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -53 41 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
76328541 104521 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 421 5 1 6 4.0 CSc1nc2c(Cc3ccccc3)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113560 104521 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 421 5 1 6 4.0 CSc1nc2c(Cc3ccccc3)cccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
16019553 10606 7 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10606 7 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322637 56377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642124 56377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
11162301 120503 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 297 4 1 6 1.7 CCCS(=O)(=O)c1c(SC)nc2ccccn2c1=N 10.1021/jm034142q
CHEMBL356540 120503 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 297 4 1 6 1.7 CCCS(=O)(=O)c1c(SC)nc2ccccn2c1=N 10.1021/jm034142q
44395451 65931 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184652 65931 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
72197484 102021 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL2393243 102021 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
CHEMBL3040324 102021 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 minsDisplacement of [3H]-LSD from human recombinant 5HT-6 receptor expressed in CHOK1 cell membranes after 60 mins
ChEMBL 330 4 2 4 3.5 c1ccc(Cc2nc3c(c(Nc4ccccc4)n2)CCNCC3)cc1 10.1016/j.ejmech.2013.02.020
46885213 8375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT6 (receptor)Inhibition of 5HT6 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 8375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of 5HT6 (receptor)Inhibition of 5HT6 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
49836386 18364 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
CHEMBL1275709 18364 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
2105 3005 34 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3005 34 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3005 34 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3005 34 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3005 34 None -19 33 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
156018343 177318 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3cc(NS(=O)(=O)c4cccc5ccccc45)ccc3s2)CC1 10.1016/j.ejmech.2018.11.017
CHEMBL4644799 177318 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 438 4 1 6 4.0 CN1CCN(c2nc3cc(NS(=O)(=O)c4cccc5ccccc45)ccc3s2)CC1 10.1016/j.ejmech.2018.11.017
10286610 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL355905 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
49864723 15515 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222363 15515 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 423 6 0 4 4.2 CCCN(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
10286610 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL355905 120351 0 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
118465027 138323 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3781617 138323 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 443 7 2 5 2.9 COc1ccc(S(=O)(=O)NCCc2cccc3cc(F)ccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
56849715 68537 3 None - 1 Human 8.4 pIC50 = 8.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922624 68537 3 None - 1 Human 8.4 pIC50 = 8.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 400 4 1 8 1.7 CNc1nn2c(N3CCN(C)CC3)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44155874 57315 15 None - 1 Human 8.3 pIC50 = 8.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57315 15 None - 1 Human 8.3 pIC50 = 8.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
53324933 57317 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668502 57317 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 319 3 0 6 2.6 CSc1nn2c(C)ccnc2c1S(=O)(=O)c1ccccc1 nan
44403351 123677 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 286 1 1 1 4.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CC2CCC(C1)N2C 10.1016/j.bmcl.2005.06.067
CHEMBL363417 123677 3 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 286 1 1 1 4.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CC2CCC(C1)N2C 10.1016/j.bmcl.2005.06.067
9921064 126657 18 None - 3 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1016/j.bmcl.2005.06.067
CHEMBL365751 126657 18 None - 3 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1016/j.bmcl.2005.06.067
44403366 167904 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 3 2 1 4.2 CCCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL435126 167904 4 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 274 3 2 1 4.2 CCCc1[nH]c2ccc(Cl)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
21512050 89273 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 260 1 1 2 3.5 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1C 10.1016/j.ejmech.2013.03.006
CHEMBL2376492 89273 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 260 1 1 2 3.5 Cc1c(C2=CCNCC2)c2cc(Cl)ccc2n1C 10.1016/j.ejmech.2013.03.006
3561 18886 34 None -3 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 18886 34 None -3 11 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
10427673 104518 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2cc(C)ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113557 104518 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 345 3 1 6 2.7 CSc1nc2cc(C)ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
53325266 56375 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 3 0 6 4.4 Cc1c(S(=O)(=O)N2CCC(=O)c3ccc(N4CCN(C)CC4)cc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.12.007
CHEMBL1642122 56375 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 3 0 6 4.4 Cc1c(S(=O)(=O)N2CCC(=O)c3ccc(N4CCN(C)CC4)cc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2010.12.007
107715 199260 18 None -29 20 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199260 18 None -29 20 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199260 18 None -29 20 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
53320011 56384 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 CC1CC(=O)c2c(N3CCNCC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642131 56384 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 CC1CC(=O)c2c(N3CCNCC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
10246904 104491 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 344 5 3 7 1.1 N=c1c(S(=O)(=O)c2ccccc2)c(NCCO)nc2ccccn12 10.1016/j.bmc.2014.01.003
CHEMBL3113363 104491 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 344 5 3 7 1.1 N=c1c(S(=O)(=O)c2ccccc2)c(NCCO)nc2ccccn12 10.1016/j.bmc.2014.01.003
10364512 104482 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 415 4 1 7 3.3 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113354 104482 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 415 4 1 7 3.3 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmc.2014.01.003
49864600 15486 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 5.0 CC(C)N(c1ccc(Oc2cccnc2)nc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
CHEMBL1222136 15486 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 6 0 5 5.0 CC(C)N(c1ccc(Oc2cccnc2)nc1)S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.150
11005810 10367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
53325265 56372 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642119 56372 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@@H]1CC(=O)c2ccc(N3CCN(C)CC3)cc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
53318267 57351 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 nan
CHEMBL1668577 57351 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 363 4 0 7 2.9 COc1ccc(S(=O)(=O)c2c(SC)nn3c(C)cc(C)nc23)cc1 nan
53326175 57354 3 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
CHEMBL1668580 57354 3 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 385 3 0 6 3.7 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(F)c(Cl)c1 nan
44476701 126899 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659968 126899 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
53317398 56382 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.7 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
CHEMBL1642129 56382 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.7 Cc1cc(N2CCN(C)CC2)c2c(c1)N(S(=O)(=O)c1ccc3ccccc3c1)CCC2=O 10.1016/j.bmcl.2010.12.007
9929665 66458 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL185958 66458 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
10385670 104517 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 389 4 1 8 2.2 COC(=O)c1ccc2nc(SC)c(S(=O)(=O)c3ccccc3)c(=N)n2c1 10.1016/j.bmc.2014.01.003
CHEMBL3113556 104517 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 389 4 1 8 2.2 COC(=O)c1ccc2nc(SC)c(S(=O)(=O)c3ccccc3)c(=N)n2c1 10.1016/j.bmc.2014.01.003
44155871 60661 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762571 60661 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
16019580 10463 2 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10463 2 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
118465046 138331 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 481 8 2 6 3.3 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCNCC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
CHEMBL3781772 138331 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 481 8 2 6 3.3 COc1ccc2cccc(C3(CNS(=O)(=O)c4ccc(OC)c(N5CCNCC5)c4)CC3)c2c1 10.1021/acsmedchemlett.5b00466
53322935 57363 3 None - 1 Human 8.3 pIC50 = 8.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
CHEMBL1668589 57363 3 None - 1 Human 8.3 pIC50 = 8.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 322 3 1 6 2.3 CNc1nn2cccnc2c1S(=O)(=O)c1cccc(Cl)c1 nan
118465021 138236 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
CHEMBL3780530 138236 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 455 8 2 6 2.8 COc1ccc(S(=O)(=O)NCCc2ccc(OC)c3ccccc23)cc1N1CCNCC1 10.1021/acsmedchemlett.5b00466
58357860 128505 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670281 128505 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 411 3 0 6 3.7 CSc1nn2c(C)c(Br)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357805 128506 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 425 5 0 7 4.7 CSc1nn2c(C)c(Oc3ccccc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL3670282 128506 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 425 5 0 7 4.7 CSc1nn2c(C)c(Oc3ccccc3)c(C)nc2c1S(=O)(=O)c1ccccc1 nan
58357740 128509 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
CHEMBL3670285 128509 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 337 3 0 6 2.7 CSc1nn2ccc(C)nc2c1S(=O)(=O)c1ccc(F)cc1 nan
44403377 124320 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 302 4 1 1 5.0 CCCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL364271 124320 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 302 4 1 1 5.0 CCCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
73351903 89265 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89265 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11741319 104481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 393 3 1 6 3.6 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1cc(C)c(Cl)cc1C 10.1016/j.bmc.2014.01.003
CHEMBL3113353 104481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 393 3 1 6 3.6 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1cc(C)c(Cl)cc1C 10.1016/j.bmc.2014.01.003
44155875 60658 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1762568 60658 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 347 4 0 6 3.3 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
46700867 175417 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
CHEMBL4588956 175417 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 minsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins
ChEMBL 377 14 1 4 5.0 CCCCCCCCCCNC(=O)/C=C/c1cc(OC)c(OC)c(OC)c1 10.1016/j.ejmech.2019.04.009
1472656 34405 22 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1429795 34405 22 None - 1 Human 6.3 pIC50 = 6.3 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
1212 1632 45 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -48 65 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
10246185 104485 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 332 3 0 6 2.2 CSc1nc2ccccn2c(=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113357 104485 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 332 3 0 6 2.2 CSc1nc2ccccn2c(=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
11414926 34157 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 285 4 1 5 2.3 N#C/C(=C\Nc1ccccn1)S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL142783 34157 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 285 4 1 5 2.3 N#C/C(=C\Nc1ccccn1)S(=O)(=O)c1ccccc1 10.1021/jm034142q
8447 188362 80 None -33 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -33 13 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
6623 162770 93 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL418971 162770 93 None - 1 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
10249280 36944 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL145304 36944 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
4543 169982 36 None -9 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -9 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -9 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
10409272 104514 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 409 3 1 6 3.1 CSc1nc2ccc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113553 104514 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 409 3 1 6 3.1 CSc1nc2ccc(Br)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
49799685 10849 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173209 10849 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
2726 906 64 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -10 72 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
10091305 104524 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 382 3 1 7 2.9 CSc1nc2c3ncccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113563 104524 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 382 3 1 7 2.9 CSc1nc2c3ncccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
53321319 56383 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 513 3 0 5 4.1 CN1CCN(c2cc(Br)cc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642130 56383 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 513 3 0 5 4.1 CN1CCN(c2cc(Br)cc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
10362440 121254 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2014.01.003
CHEMBL358948 121254 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmc.2014.01.003
CHEMBL508338 188379 0 None -95 6 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
49864289 15416 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1221449 15416 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 6 0 4 4.2 CN1CCN(c2cccc(N(CC3CC3)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
7184883 10795 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10795 3 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
7185123 10577 7 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10577 7 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44403376 133057 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.6 CCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL371203 133057 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.6 CCCN1CC=C(c2c(C)[nH]c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2005.06.067
10341241 104492 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 405 4 2 7 3.4 Cc1ccc(Nc2nc3ccc(C)cn3c(=N)c2S(=O)(=O)c2ccccc2)nc1 10.1016/j.bmc.2014.01.003
CHEMBL3113364 104492 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 405 4 2 7 3.4 Cc1ccc(Nc2nc3ccc(C)cn3c(=N)c2S(=O)(=O)c2ccccc2)nc1 10.1016/j.bmc.2014.01.003
10094519 104523 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 435 5 1 6 4.3 CSc1nc2c(C)cc(Cc3ccccc3)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113562 104523 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 435 5 1 6 4.3 CSc1nc2c(C)cc(Cc3ccccc3)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
44403386 70233 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 336 3 1 1 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL194908 70233 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 336 3 1 1 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2005.06.067
53320010 56370 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642117 56370 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
16019573 10892 10 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173579 10892 10 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
161 743 3 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 743 3 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 743 3 None -12 6 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
49864602 15488 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
CHEMBL1222138 15488 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 5 0 4 3.0 CC(C)N(c1cccc(N2CCN(C)CC2)c1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.06.150
7184886 10506 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10506 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
10452816 104480 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 387 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1016/j.bmc.2014.01.003
CHEMBL3113352 104480 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 387 3 1 6 3.7 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc(C(C)(C)C)cc1 10.1016/j.bmc.2014.01.003
194 3451 25 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
443391 3451 25 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
CHEMBL14460 3451 25 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptorDisplacement of [3H]LSD from human cloned 5HT6 receptor
ChEMBL 428 3 1 4 5.5 O=C(N1CCc2c1cc(c(c2)C)C(F)(F)F)Nc1ccc(nc1)Oc1cccnc1C 10.1016/j.bmcl.2008.06.064
10249280 36944 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL145304 36944 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2c3ccccc3ccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
56849580 68533 4 None - 1 Human 7.2 pIC50 = 7.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1922620 68533 4 None - 1 Human 7.2 pIC50 = 7.2 Binding
Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Assay: Screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out by method of radioligand binding. For this purpose membrane species were prepared from expressing recombinant human 5-HT6 receptors HeLa cells by means of their homogenization in glass homogenizer with subsequent separation of plasmatic membranes from cell nucli, mitochondria's and cell wreckages by differential centrifugation. Determination of tested compounds binding to 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 388 7 2 8 1.9 CNc1nn2c(NCCN(C)C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
42635388 187115 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
CHEMBL495250 187115 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 471 8 1 5 3.6 COc1ccc(S(=O)(=O)NC(C)CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1 10.1016/j.bmc.2008.04.023
49864722 15514 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
CHEMBL1222362 15514 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 4 0 4 3.4 CN1CCN(c2cccc(N(C)S(=O)(=O)c3ccc4ccccc4c3)c2)CC1 10.1016/j.bmcl.2010.06.150
53325267 56378 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642125 56378 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 C[C@H]1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
44476607 81940 2 None - 1 Human 8.2 pIC50 = 8.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172192 81940 2 None - 1 Human 8.2 pIC50 = 8.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
10131112 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
10131112 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1523 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
16019292 10891 7 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10891 7 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44403384 132754 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.5 CCc1[nH]c2ccc(Cl)cc2c1C1=CCN(CC)CC1 10.1016/j.bmcl.2005.06.067
CHEMBL370436 132754 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 288 3 1 1 4.5 CCc1[nH]c2ccc(Cl)cc2c1C1=CCN(CC)CC1 10.1016/j.bmcl.2005.06.067
10021389 32717 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1021/jm034142q
CHEMBL141549 32717 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1021/jm034142q
73356443 89271 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376490 89271 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11740084 104519 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 5 1 6 3.3 CCCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
CHEMBL3113558 104519 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 5 1 6 3.3 CCCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
100 3745 52 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -17 55 Human 7.2 pIC50 = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
45278805 7369 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086754 7369 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
191 399 92 None -20 28 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -20 28 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -20 28 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -20 28 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -20 28 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
58149665 81932 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172183 81932 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
42635387 187109 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
CHEMBL495212 187109 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 477 7 1 4 4.6 O=S(=O)(NCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2008.04.023
26987 936 29 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -58 21 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
11730467 10925 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10925 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
108029 3361 50 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
23 3361 50 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL18785 3361 50 None -630 13 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.bmcl.2005.06.067
10362440 121254 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm034142q
CHEMBL358948 121254 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 381 3 1 6 3.5 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm034142q
12147017 165505 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL425714 165505 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assayInhibitory concentration against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells in cAMP assay
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
51003551 56376 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642123 56376 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
44388701 122619 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL361213 122619 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human recombinant 5HT6 receptor expressed in CHO cellsInhibition of human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
9976690 104516 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 374 4 2 7 1.5 CSc1nc2ccc(C(N)=O)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113555 104516 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 374 4 2 7 1.5 CSc1nc2ccc(C(N)=O)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
3066250 69943 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 69943 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
73351911 89275 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 3 1 2 4.4 CCCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
CHEMBL2376560 89275 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 288 3 1 2 4.4 CCCn1c(C)c(C2=CCNCC2)c2cc(Cl)ccc21 10.1016/j.ejmech.2013.03.006
10021389 32717 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
CHEMBL141549 32717 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 359 4 1 6 2.9 CCc1ccn2c(=N)c(S(=O)(=O)c3ccccc3)c(SC)nc2c1 10.1016/j.bmc.2014.01.003
59636981 125315 3 None - 0 Human 7.1 pIC50 = 7.1 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 361 4 0 6 3.6 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(C)cc1 nan
CHEMBL3648342 125315 3 None - 0 Human 7.1 pIC50 = 7.1 Binding
Functional Assay: Functional assay using 5-HT6 receptors.Functional Assay: Functional assay using 5-HT6 receptors.
ChEMBL 361 4 0 6 3.6 CCSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccc(C)cc1 nan
3066250 69943 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 69943 2 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
10907460 9735 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9735 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human 5-hydroxytryptamine 6 receptorInhibition of human 5-hydroxytryptamine 6 receptor
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44476801 81937 2 None - 1 Human 6.1 pIC50 = 6.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172189 81937 2 None - 1 Human 6.1 pIC50 = 6.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
10090742 104484 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 3 0 6 2.3 CSc1nc2ccccn2/c(=N\C(C)=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
CHEMBL3113356 104484 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells
ChEMBL 373 3 0 6 2.3 CSc1nc2ccccn2/c(=N\C(C)=O)c1S(=O)(=O)c1ccccc1 10.1016/j.bmc.2014.01.003
135 2496 38 None -21 57 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -21 57 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -21 57 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -21 57 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -21 57 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
12 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
12 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
6918513 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
CHEMBL267615 1524 14 None 6 7 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against 5-hydroxytryptamine 6 receptor in humanInhibitory activity against 5-hydroxytryptamine 6 receptor in human
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.06.067
10247229 120533 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
CHEMBL356781 120533 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligandBinding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand
ChEMBL 349 3 1 6 2.5 CSc1nc2ccc(F)cn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm034142q
6758 166563 73 None - 1 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
CHEMBL429023 166563 73 None - 1 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
4011 81996 43 None -28 23 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -28 23 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
73354883 89269 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 349 4 2 4 4.6 Cc1[nH]c2ccc(Oc3ccccc3[N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376488 89269 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 349 4 2 4 4.6 Cc1[nH]c2ccc(Oc3ccccc3[N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
51003586 56379 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 4 0 5 4.2 CCC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642126 56379 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 463 4 0 5 4.2 CCC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
22424009 10852 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 5 1 8 3.4 CCC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173211 10852 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 5 1 8 3.4 CCC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
44403335 69936 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 256 3 2 2 3.1 CCc1[nH]c2ccc(OC)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
CHEMBL194248 69936 4 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cellsDisplacement of [3H]LSD binding to cloned h5-HT6 receptors stably expressed in HEK cells
ChEMBL 256 3 2 2 3.1 CCc1[nH]c2ccc(OC)cc2c1C1=CCNCC1 10.1016/j.bmcl.2005.06.067
45482789 197247 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 197247 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
20901207 10882 0 None - 1 Human 7.0 pIC50 = 7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10882 0 None - 1 Human 7.0 pIC50 = 7 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
165193 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3138 60 None -158 42 Human 6.0 pIC50 = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
6918689 85557 3 None 812 2 Human 8.5 pKd = 8.5 Binding
Antagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsAntagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
CHEMBL23038 85557 3 None 812 2 Human 8.5 pKd = 8.5 Binding
Antagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsAntagonism assessed in a functional cAMP binding assay using 5-CT to stimulate human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
6918786 113669 1 None - 1 Human 10.4 pKi = 10.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 425 3 1 4 3.2 O=S(=O)(c1cccc(Cl)c1Cl)N1CCc2c(cccc2N2CCNCC2)C1 10.1021/jm5003952
CHEMBL3329438 113669 1 None - 1 Human 10.4 pKi = 10.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 425 3 1 4 3.2 O=S(=O)(c1cccc(Cl)c1Cl)N1CCc2c(cccc2N2CCNCC2)C1 10.1021/jm5003952
57412089 131254 0 None - 1 Human 10.3 pKi = 10.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692995 131254 0 None - 1 Human 10.3 pKi = 10.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
46889326 6937 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 340 3 2 3 3.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3c[nH]c4ccccc34)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084794 6937 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 340 3 2 3 3.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3c[nH]c4ccccc34)ccc21 10.1016/j.bmcl.2010.03.110
46889856 7091 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 329 4 0 3 3.5 CN(C)CC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085462 7091 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 329 4 0 3 3.5 CN(C)CC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
22557235 153037 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 3 1 5 3.0 O=S(=O)(c1c(Cl)cccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL398034 153037 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 3 1 5 3.0 O=S(=O)(c1c(Cl)cccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
46889893 7286 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 319 3 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086326 7286 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 319 3 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
68109141 131141 0 None - 1 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 3 2 5 3.4 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692882 131141 0 None - 1 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 3 2 5 3.4 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(oc12)CCNC3 nan
118181414 190601 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5189271 190601 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44156628 6636 3 None 2630 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083654 6636 3 None 2630 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 328 3 1 6 2.1 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
164616201 184249 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 467 11 2 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4852099 184249 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 467 11 2 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113783
46890192 7016 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 5 2 4 2.2 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085120 7016 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 5 2 4 2.2 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890322 7137 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 1 4 2.8 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CC(O)C1 10.1016/j.bmcl.2010.03.110
CHEMBL1085658 7137 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 1 4 2.8 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CC(O)C1 10.1016/j.bmcl.2010.03.110
11654245 7237 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 401 4 2 5 2.2 O=C1CN=C(NC[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)N1 10.1016/j.bmcl.2010.03.110
CHEMBL1086113 7237 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 401 4 2 5 2.2 O=C1CN=C(NC[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)N1 10.1016/j.bmcl.2010.03.110
46889328 7266 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 6 2 4 2.2 NC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086252 7266 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 6 2 4 2.2 NC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10182243 130141 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL368209 130141 0 None - 1 Human 10.0 pKi = 10 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
68115723 131249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(oc12)CCNC3 nan
CHEMBL3692990 131249 0 None - 1 Human 10.0 pKi = 10 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(oc12)CCNC3 nan
57414386 131227 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692968 131227 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
68115821 131252 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 3 1 5 3.7 COc1cc(S(=O)(=O)c2cc(F)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692993 131252 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 3 1 5 3.7 COc1cc(S(=O)(=O)c2cc(F)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115733 131731 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 1 5 3.3 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696966 131731 0 None - 1 Human 10.0 pKi = 10.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 1 5 3.3 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44156754 6432 3 None 891 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082763 6432 3 None 891 2 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
10982183 92788 0 None 177 3 Human 9.9 pKi = 9.9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 396 3 2 6 1.7 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCNCC3)c2)cc1 10.1021/jm021085c
CHEMBL24474 92788 0 None 177 3 Human 9.9 pKi = 9.9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 396 3 2 6 1.7 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCNCC3)c2)cc1 10.1021/jm021085c
68109407 131125 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 1 5 2.9 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692867 131125 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 1 5 2.9 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44398571 123851 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 382 4 0 5 3.4 CON1CCN(c2ccc(S(=O)(=O)c3cccc4ccccc34)cc2)CC1 10.1021/jm050247c
CHEMBL363792 123851 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 382 4 0 5 3.4 CON1CCN(c2ccc(S(=O)(=O)c3cccc4ccccc34)cc2)CC1 10.1021/jm050247c
6918745 126528 1 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 341 3 2 4 2.4 O=S(=O)(c1ccccc1)c1cc2c(N3CCNCC3)cccc2[nH]1 10.1021/jm050247c
CHEMBL365569 126528 1 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 341 3 2 4 2.4 O=S(=O)(c1ccccc1)c1cc2c(N3CCNCC3)cccc2[nH]1 10.1021/jm050247c
46890190 6724 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083886 6724 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890264 6918 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 398 5 2 4 1.9 NS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084711 6918 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 398 5 2 4 1.9 NS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889350 7004 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 363 6 2 4 2.7 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
CHEMBL1085037 7004 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 363 6 2 4 2.7 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
68115629 131169 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 2 4 4.0 O=S(=O)(c1ccc2[nH]ccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692910 131169 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 2 4 4.0 O=S(=O)(c1ccc2[nH]ccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116227 131233 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692974 131233 0 None - 1 Human 9.9 pKi = 9.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
68108832 131153 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131153 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
46890324 6830 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 381 6 2 4 2.8 O=S(=O)(c1cccc(F)c1)c1cc(F)c2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
CHEMBL1084336 6830 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 381 6 2 4 2.8 O=S(=O)(c1cccc(F)c1)c1cc(F)c2c(c1)CCC[C@H]2CNCCO 10.1016/j.bmcl.2010.03.110
46890884 7113 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085585 7113 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889918 7121 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 4 2 3 2.5 CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085617 7121 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 4 2 3 2.5 CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
11595360 7228 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 343 4 3 3 2.4 N=C(N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086079 7228 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 343 4 3 3 2.4 N=C(N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46889890 7283 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 301 3 1 3 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086323 7283 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 301 3 1 3 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
22557241 149052 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 6 1.8 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL394690 149052 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 6 1.8 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
68115724 131247 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 3 1 6 3.4 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(oc12)CCNC3 nan
CHEMBL3692988 131247 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 3 1 6 3.4 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(oc12)CCNC3 nan
68115722 131248 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692989 131248 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 4.1 COc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
11256720 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
9444 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
CHEMBL1083390 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
DB12680 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
11256720 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
9444 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
CHEMBL1083390 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
DB12680 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003759
68108708 131121 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 400 2 1 5 4.1 Cn1cc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
CHEMBL3692863 131121 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 400 2 1 5 4.1 Cn1cc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
68115667 131256 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2cccs2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692997 131256 0 None - 1 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2cccs2)cc2c3c(oc12)CCNC3 nan
118173772 189781 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5177311 189781 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115716 131230 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
CHEMBL3692971 131230 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
68116278 131234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692975 131234 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
24873459 135011 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 399 5 3 3 4.3 NCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm050247c
CHEMBL372879 135011 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 399 5 3 3 4.3 NCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm050247c
44398389 135733 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 429 3 0 5 4.4 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4C=CCC4C3)cc21 10.1021/jm050247c
CHEMBL373322 135733 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 429 3 0 5 4.4 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4C=CCC4C3)cc21 10.1021/jm050247c
46220503 6379 4 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 362 4 2 3 2.7 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082508 6379 4 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 362 4 2 3 2.7 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
11639865 6677 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 397 5 1 4 2.6 CS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083781 6677 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 397 5 1 4 2.6 CS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890325 6898 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 380 4 2 3 2.9 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1084603 6898 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 380 4 2 3 2.9 NC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
6918751 113661 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 2 4 3.7 O=S(=O)(c1cc2cccc(N3CCNCC3)c2[nH]1)c1cccc(Cl)c1Cl 10.1021/jm5003952
CHEMBL3329430 113661 2 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 2 4 3.7 O=S(=O)(c1cc2cccc(N3CCNCC3)c2[nH]1)c1cccc(Cl)c1Cl 10.1021/jm5003952
11652654 113673 0 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 4 1 5 1.9 CNC[C@@H]1COc2ccc(S(=O)(=O)c3ccccc3)cc2O1 10.1021/jm5003952
CHEMBL3329442 113673 0 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 4 1 5 1.9 CNC[C@@H]1COc2ccc(S(=O)(=O)c3ccccc3)cc2O1 10.1021/jm5003952
10019089 113682 1 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 323 3 1 4 2.0 O=C1COc2c(N3CCNCC3)cccc2N1Cc1ccccc1 10.1021/jm5003952
CHEMBL3329451 113682 1 None - 1 Human 9.7 pKi = 9.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 323 3 1 4 2.0 O=C1COc2c(N3CCNCC3)cccc2N1Cc1ccccc1 10.1021/jm5003952
145954675 162128 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 362 3 1 3 3.0 CN(C(N)=O)[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4170220 162128 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 362 3 1 3 3.0 CN(C(N)=O)[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.ejmech.2017.12.053
6918715 91491 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrsDisplacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrs
ChEMBL 407 3 1 5 2.6 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1Cl)CCO2 10.1016/j.bmc.2013.05.040
CHEMBL2413982 91491 1 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrsDisplacement of [3H]-lysergic acid diethylamide from human 5-HT6 receptor expressed in HEK293 cell membranes after 3.5 hrs
ChEMBL 407 3 1 5 2.6 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1Cl)CCO2 10.1016/j.bmc.2013.05.040
9910619 176343 7 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL46187 176343 7 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
44516817 57358 4 None 4365 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668584 57358 4 None 4365 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 316 3 1 6 2.2 CNc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
6918836 60217 15 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm049615n
CHEMBL175835 60217 15 None - 1 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm049615n
68108410 131122 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 1 5 3.9 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
CHEMBL3692864 131122 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 386 2 1 5 3.9 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
68115714 131232 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692973 131232 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
44156752 6502 3 None 645 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
CHEMBL1083075 6502 3 None 645 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.4 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1021/jm100350r
118181460 189301 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5169546 189301 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 405 4 1 6 3.0 COc1ccc(S(=O)(=O)n2ccc3ccc(Cl)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
72549033 110204 0 None 562 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260311 110204 0 None 562 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 367 3 0 5 3.3 CN1CCC(c2cccc3cc(S(=O)(=O)c4ccccn4)cnc23)CC1 10.1021/ml500045k
68109211 131124 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692866 131124 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
68116231 131718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.2 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696953 131718 0 None - 1 Human 9.7 pKi = 9.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.2 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2013.05.040
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.6b01662
68115666 131255 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 4.2 COc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692996 131255 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 4.2 COc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115858 131721 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 5 4.4 Cc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696956 131721 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 5 4.4 Cc1cc(S(=O)(=O)c2ccc3sccc3c2)cc2c3c(oc12)CCNC3 nan
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm100350r
11256720 2024 73 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
9444 2024 73 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
CHEMBL1083390 2024 73 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
DB12680 2024 73 None 1 6 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acsmedchemlett.6b00056
53323402 59826 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642864 59826 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739646 59826 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(CN3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/jm5003952
46780481 107045 18 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
9903970 107045 18 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
CHEMBL3187365 107045 18 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
CHEMBL3544974 107045 18 None -8 53 Human 9.6 pKi = 9.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1021/jm5003952
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmcl.2021.128275
68109588 131160 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CCNCC3 nan
CHEMBL3692901 131160 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CCNCC3 nan
46890326 6899 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 395 5 2 4 2.3 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1084604 6899 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 395 5 2 4 2.3 O=C(CO)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)cc(F)c21 10.1016/j.bmcl.2010.03.110
46889351 7005 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 7 1 4 3.3 COCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085038 7005 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 7 1 4 3.3 COCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889891 7284 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 317 3 2 4 2.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(O)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086324 7284 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 317 3 2 4 2.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(O)c3)ccc21 10.1016/j.bmcl.2010.03.110
10270854 71331 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196410 71331 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
46867521 6431 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082762 6431 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
58258774 128451 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128451 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
118181454 189368 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5170650 189368 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
118173755 191736 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206617 191736 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
44327759 206175 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL96745 206175 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115757 131201 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1csc2ccccc12 nan
CHEMBL3692942 131201 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1csc2ccccc12 nan
68115754 131251 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccsc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692992 131251 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccsc2)cc2c3c(oc12)CCNC3 nan
52914691 70429 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70429 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
57394334 70430 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950776 70430 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
11256720 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2024 73 None -1 6 Human 9.6 pKi = 9.6 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
52914691 70429 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70429 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57394334 70430 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70430 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115840 131253 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692994 131253 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
68115738 131259 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3693000 131259 0 None - 1 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
58258777 128458 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 2 1 5 4.9 Cc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669657 128458 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 2 1 5 4.9 Cc1cc(S(=O)(=O)c2csc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
10027190 119896 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 458 7 0 7 3.9 COc1ccc(OC)c(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)c1 10.1016/j.bmcl.2004.01.071
CHEMBL353552 119896 0 None - 1 Human 9.5 pKi = 9.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 458 7 0 7 3.9 COc1ccc(OC)c(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)c1 10.1016/j.bmcl.2004.01.071
9822810 69159 0 None 6 2 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1021/jm5003952
CHEMBL193400 69159 0 None 6 2 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1021/jm5003952
11569025 113683 0 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 471 3 1 4 5.2 O=C1c2cccc(N3CCNCC3)c2Oc2ccc(F)cc2N1Cc1cccc(C(F)(F)F)c1 10.1021/jm5003952
CHEMBL3329452 113683 0 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 471 3 1 4 5.2 O=C1c2cccc(N3CCNCC3)c2Oc2ccc(F)cc2N1Cc1cccc(C(F)(F)F)c1 10.1021/jm5003952
11587610 113684 3 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 3 2 4 1.8 O=c1[nH]c2c(N3CCNCC3)cccc2n1Cc1ccccc1 10.1021/jm5003952
CHEMBL3329453 113684 3 None - 1 Human 9.5 pKi = 9.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 3 2 4 1.8 O=c1[nH]c2c(N3CCNCC3)cccc2n1Cc1ccccc1 10.1021/jm5003952
11624561 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL187865 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL194307 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
9840981 162100 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4169827 162100 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
44327759 206175 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1021/jm030030n
CHEMBL96745 206175 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 4 1 6 3.1 COc1ccc(S(=O)(=O)n2ccc3ccc(Br)cc32)cc1N1CCNCC1 10.1021/jm030030n
10154392 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL370779 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2020.112765
4106 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
5358812 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
89 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
CHEMBL93240 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113783
10154392 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL370779 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2016.08.016
4106 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
5358812 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
89 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
CHEMBL93240 2466 16 None -1 33 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2021.113792
164610804 184504 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 9 2 6 4.0 CC(=O)Nc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4855991 184504 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 9 2 6 4.0 CC(=O)Nc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
11624561 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL187865 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL194307 69944 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
9950255 195140 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565723 195140 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 349 5 1 5 2.7 CNCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
9956634 63156 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 475 8 2 4 6.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
CHEMBL179926 63156 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 475 8 2 4 6.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
11363934 200557 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
CHEMBL609994 200557 0 None - 1 Human 9.5 pKi = 9.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 5 2 3 4.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(I)cc3)cc12 10.1021/jm049243i
118010064 131719 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 5 3.8 Cc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696954 131719 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 5 3.8 Cc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(oc12)CCNC3 nan
58258781 128462 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 2 5 3.9 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669661 128462 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 2 5 3.9 COc1cc(S(=O)(=O)c2ccc3[nH]ccc3c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258821 128488 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669687 128488 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
17940125 120395 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL356021 120395 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3ccc(Br)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10413595 161292 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161292 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10413595 161292 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1021/jm050247c
CHEMBL414628 161292 0 None 1 11 Human 9.5 pKi = 9.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1021/jm050247c
11682024 6440 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)cc(F)c21 10.1016/j.bmcl.2010.03.110
CHEMBL1082777 6440 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 361 4 1 3 3.2 CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3ccccc3)cc(F)c21 10.1016/j.bmcl.2010.03.110
11515192 7012 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.2 CNCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085111 7012 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.2 CNCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46889917 7073 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 290 3 2 3 2.2 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085372 7073 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 290 3 2 3 2.2 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
46889353 7311 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 5 2 4 2.2 NCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086477 7311 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 5 2 4 2.2 NCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
17978373 69469 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)ccc(Cl)c21 10.1016/j.bmcl.2005.06.107
CHEMBL193629 69469 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)ccc(Cl)c21 10.1016/j.bmcl.2005.06.107
10154392 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL370779 132993 8 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
17978408 133096 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371375 133096 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1cc(Cl)c2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
10134086 165357 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 2 4 3.1 O=S(=O)(c1cccc(Cl)c1)c1c[nH]c2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL425015 165357 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 2 4 3.1 O=S(=O)(c1cccc(Cl)c1)c1c[nH]c2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
11407072 93239 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 405 3 1 5 2.6 CC1(C)CN(S(=O)(=O)c2ccccc2F)c2cccc(N3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL246918 93239 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 405 3 1 5 2.6 CC1(C)CN(S(=O)(=O)c2ccccc2F)c2cccc(N3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
52914691 70429 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70429 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
52914691 70429 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70429 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115828 131228 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692969 131228 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
68115806 131244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 441 4 2 6 3.5 COc1cc(S(=O)(=O)c2cccc(C(O)C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692985 131244 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 441 4 2 6 3.5 COc1cc(S(=O)(=O)c2cccc(C(O)C(F)(F)F)c2)cc2c3c(oc12)CCNC3 nan
58258771 128441 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 2 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669640 128441 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 2 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
118181455 190471 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5187350 190471 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3ccc(Br)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
57394334 70430 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70430 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115726 131250 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692991 131250 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 5 3.2 COc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
68115779 131732 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 4 1 5 3.5 O=S(=O)(c1ccccc1)c1cc(OC(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696967 131732 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 4 1 5 3.5 O=S(=O)(c1ccccc1)c1cc(OC(F)F)c2oc3c(c2c1)CNCC3 nan
10172764 110205 7 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
CHEMBL3260313 110205 7 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
CHEMBL5201619 110205 7 None -2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/ml500045k
58258774 128451 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128451 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258788 128491 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669690 128491 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
68108997 131117 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cccc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692859 131117 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cccc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68108832 131153 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131153 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
68115721 131243 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(C(C)(C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692984 131243 0 None - 1 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(C(C)(C)O)c2)cc2c3c(oc12)CCNC3 nan
57394334 70430 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950776 70430 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 nan
57394334 70430 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950776 70430 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115660 131245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
52914691 70429 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950775 70429 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
52914691 70429 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950775 70429 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44476436 81935 5 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172186 81935 5 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
44476436 81935 5 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172186 81935 5 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
68108513 131118 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692860 131118 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115756 131258 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
CHEMBL3692999 131258 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(oc12)CCNC3 nan
46890157 6380 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 2 3 3.0 CNC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082509 6380 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 2 3 3.0 CNC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890221 6678 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 411 5 0 4 3.0 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(C)(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1083782 6678 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 411 5 0 4 3.0 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(C)(=O)=O 10.1016/j.bmcl.2010.03.110
46890155 6774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 404 6 1 4 2.8 CN(C)CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084071 6774 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 404 6 1 4 2.8 CN(C)CC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889892 7285 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 2.9 COc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1086325 7285 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 2.9 COc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
10156341 134722 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL372513 134722 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
44403305 135090 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.107
CHEMBL372929 135090 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1016/j.bmcl.2005.06.107
17960999 93141 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 391 3 1 5 2.1 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246499 93141 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 391 3 1 5 2.1 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
11697242 93190 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 3 1 5 2.5 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246705 93190 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 3 1 5 2.5 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
22557272 93191 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 389 4 1 6 1.7 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246706 93191 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 389 4 1 6 1.7 COc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
11631819 113672 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)OCCC2N1CCNCC1 10.1021/jm5003952
CHEMBL3329441 113672 0 None - 1 Human 9.4 pKi = 9.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 2.2 O=S(=O)(c1ccccc1)c1ccc2c(c1)OCCC2N1CCNCC1 10.1021/jm5003952
44389003 123318 0 None 954 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362487 123318 0 None 954 4 Human 9.4 pKi = 9.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
46227395 198445 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL596199 198445 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
4106 2466 16 None -1 33 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 2466 16 None -1 33 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 2466 16 None -1 33 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 2466 16 None -1 33 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
164611660 184155 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccn3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4850738 184155 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccn3)cccc21 10.1016/j.ejmech.2021.113792
11566597 72649 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 3 2 6 1.9 Nc1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL200795 72649 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 3 2 6 1.9 Nc1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2005.08.059
71151933 117737 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 558 9 1 7 4.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409238 117737 0 None 3 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 558 9 1 7 4.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
10112810 63009 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 7 2 3 4.7 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
CHEMBL179408 63009 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 7 2 3 4.7 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
11384146 200048 0 None 6 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 200048 0 None 6 9 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
11351089 200051 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606559 200051 0 None - 1 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
118010063 123941 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2ccc(OC(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3639918 123941 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 409 5 1 6 3.5 COc1cc(S(=O)(=O)c2ccc(OC(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115868 131727 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 2 1 6 3.3 Cn1cc(S(=O)(=O)c2cc(C#N)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
CHEMBL3696962 131727 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 2 1 6 3.3 Cn1cc(S(=O)(=O)c2cc(C#N)c3oc4c(c3c2)CNCC4)c2ccccc21 nan
57403058 70431 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL1950777 70431 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
68115660 131245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131245 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
58258772 127422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258774 128451 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669650 128451 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 4 4.2 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
68109265 131114 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 366 2 1 5 3.6 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)c2ccccc12 nan
CHEMBL3692856 131114 0 None - 1 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 366 2 1 5 3.6 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)c2ccccc12 nan
58258763 128490 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669689 128490 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
118654432 190884 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5193483 190884 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
118173792 191820 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5208122 191820 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
155557005 173961 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4555868 173961 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
44155109 8090 3 None - 1 Human 9.4 pKi = 9.4 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091919 8090 3 None - 1 Human 9.4 pKi = 9.4 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44155109 8090 3 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091919 8090 3 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
44156863 7995 0 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
CHEMBL1091206 7995 0 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 nan
44156863 7995 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091206 7995 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 345 3 0 6 2.8 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.02.046
58258753 128482 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669681 128482 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
118654422 191727 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5206470 191727 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
118181441 191693 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5206037 191693 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 439 5 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(F)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
58258878 128440 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 2 2 4 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(C(F)(F)F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669639 128440 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 2 2 4 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(C(F)(F)F)c5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
58258780 128456 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 2 1 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)cc(F)c31)C1CCC(C2)N1 nan
CHEMBL3669655 128456 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 2 1 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4csc5ccccc45)cc(F)c31)C1CCC(C2)N1 nan
68109652 131116 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692858 131116 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115692 131225 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)CCOC3)cc2c3c(oc12)CCNC3 nan
CHEMBL3692966 131225 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)CCOC3)cc2c3c(oc12)CCNC3 nan
44156756 6503 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1083076 6503 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 2.8 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
68116229 131229 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2ccc(C(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692970 131229 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 411 3 1 5 3.9 COc1cc(S(=O)(=O)c2ccc(C(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115660 131245 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692986 131245 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2cccc(C3CCOC3)c2)cc2c3c(oc12)CCNC3 nan
46867519 6430 3 None 331 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
CHEMBL1082761 6430 3 None 331 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 342 3 1 6 2.5 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1021/jm100350r
6918682 113660 28 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 355 3 1 4 2.8 CN1CCN(c2cccc3c(S(=O)(=O)c4ccccc4)c[nH]c23)CC1 10.1021/jm5003952
CHEMBL3329429 113660 28 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 355 3 1 4 2.8 CN1CCN(c2cccc3c(S(=O)(=O)c4ccccc4)c[nH]c23)CC1 10.1021/jm5003952
10178788 134728 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1021/jm5003952
CHEMBL372537 134728 0 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1021/jm5003952
58258778 127405 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127405 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
58258755 128475 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669674 128475 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
58258797 128483 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669682 128483 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
134131472 141646 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.bmcl.2021.127909
CHEMBL3883955 141646 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.bmcl.2021.127909
46203710 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL3329435 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
164625599 185177 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 10 1 7 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1OC 10.1016/j.ejmech.2021.113792
CHEMBL4866390 185177 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 10 1 7 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1OC 10.1016/j.ejmech.2021.113792
164622030 185516 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 8 1 7 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc4c(c3)OCCO4)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4871652 185516 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 8 1 7 3.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc4c(c3)OCCO4)cccc21 10.1016/j.ejmech.2021.113792
23624307 191808 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520795 191808 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
134131472 141646 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.ejmech.2016.09.008
CHEMBL3883955 141646 0 None -1 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1c(F)cccc1F 10.1016/j.ejmech.2016.09.008
10278839 63008 0 None - 1 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 503 10 2 4 6.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
CHEMBL179407 63008 0 None - 1 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 503 10 2 4 6.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc12 10.1021/jm049615n
68115836 131717 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696952 131717 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
18354536 48339 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155717 48339 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940169 50315 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3c(Cl)ccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157454 50315 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3c(Cl)ccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940215 119094 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2cccc(I)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346338 119094 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2cccc(I)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9889681 206323 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 206323 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
9889681 206323 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 206323 0 None 316 5 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
46889895 7072 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 324 3 1 4 3.5 N#Cc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3C=N)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085368 7072 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 324 3 1 4 3.5 N#Cc1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3C=N)c1 10.1016/j.bmcl.2010.03.110
44403327 70235 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 6 2.3 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL194915 70235 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 6 2.3 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10178788 134728 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL372537 134728 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 1 5 3.1 O=S(=O)(c1ccccc1)c1csc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
20765669 93078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 8 1.9 O=S(=O)(c1cccc2nonc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246291 93078 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 8 1.9 O=S(=O)(c1cccc2nonc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
168285508 191080 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 373 3 1 5 2.7 Cc1cn(S(=O)(=O)c2cccc(F)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmc.2022.116950
CHEMBL5196479 191080 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 373 3 1 5 2.7 Cc1cn(S(=O)(=O)c2cccc(F)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmc.2022.116950
25117676 198775 0 None 831 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598444 198775 0 None 831 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
118654426 190395 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5186310 190395 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
46203710 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL3329435 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258769 128479 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 128479 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258817 128486 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669685 128486 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
46203710 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2021.128275
CHEMBL3329435 113666 2 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 356 3 1 6 2.0 Cc1nc2c(N3CCNCC3)cccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2021.128275
44155107 7996 3 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091207 7996 3 None - 1 Human 9.3 pKi = 9.3 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
44155107 7996 3 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091207 7996 3 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
118181437 191515 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5203370 191515 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 499 5 1 6 4.0 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68109001 131115 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692857 131115 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414668 131202 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1ccc2sccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692943 131202 0 None - 1 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 4.8 O=S(=O)(c1ccc2sccc2c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58258837 128457 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 2 1 5 4.2 Cc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669656 128457 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 2 1 5 4.2 Cc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258776 128484 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669683 128484 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258836 127421 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127421 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258802 128492 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669691 128492 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
10202564 1496 8 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
3217 1496 8 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
CHEMBL362628 1496 8 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmcl.2021.128275
68109317 131112 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 352 2 1 5 3.3 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
CHEMBL3692854 131112 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 352 2 1 5 3.3 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccccc21 nan
58258778 127405 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127405 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
11465618 101926 18 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 101926 18 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 101926 18 None -2 19 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
68115815 131749 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 358 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCC(O)C3 nan
CHEMBL3696984 131749 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 358 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCC(O)C3 nan
23844114 205784 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.05.076
CHEMBL94569 205784 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.05.076
23872164 9454 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 371 7 1 5 3.3 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL112296 9454 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 371 7 1 5 3.3 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
6918648 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm030030n
CHEMBL29846 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm030030n
10250472 110864 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 401 8 1 6 3.4 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL326937 110864 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 401 8 1 6 3.4 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
16117153 59823 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642889 59823 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739616 59823 0 None 1122 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1ccc2ccccc2c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
9802776 101286 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL299822 101286 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
25263305 183636 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 3.6 Cc1c(OCc2cccc(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483358 183636 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 3.6 Cc1c(OCc2cccc(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
68115787 131239 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc(C(C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692980 131239 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc(C(C)O)c2)cc2c3c(oc12)CCNC3 nan
46224879 199862 3 None -2 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL605405 199862 3 None -2 7 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 302 2 0 2 4.6 Cc1ccc2c(c1)c1c(n2/C=C\c2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
46889858 7014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2021.128275
CHEMBL1085113 7014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2021.128275
9954121 95959 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL261917 95959 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
17940212 118953 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL345110 118953 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918648 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
6918648 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL29846 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/j.bmcl.2010.12.007
9954121 95959 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL261917 95959 0 None 1258 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
276 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
5312149 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
CHEMBL431298 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2017.04.033
46890156 6617 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 389 4 3 4 2.5 N=C(N)NC(=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083575 6617 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 389 4 3 4 2.5 N=C(N)NC(=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889858 7014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085113 7014 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 344 4 2 3 2.6 NC(=O)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
46890295 7133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 416 5 2 4 2.9 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)[C@H]1CCCN1 10.1016/j.bmcl.2010.03.110
CHEMBL1085651 7133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 416 5 2 4 2.9 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)[C@H]1CCCN1 10.1016/j.bmcl.2010.03.110
11688736 7230 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 342 4 2 3 3.5 CC(=N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086080 7230 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 342 4 2 3 3.5 CC(=N)NCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
44403304 69809 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmcl.2005.06.107
CHEMBL194039 69809 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.3 Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c12 10.1016/j.bmcl.2005.06.107
20765664 93140 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 444 3 1 6 2.9 O=S(=O)(c1cccc2cccnc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246498 93140 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 444 3 1 6 2.9 O=S(=O)(c1cccc2cccnc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
17961002 93189 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 3 1 5 2.0 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(F)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL246704 93189 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 395 3 1 5 2.0 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cc(F)cc21 10.1016/j.bmcl.2006.12.093
11200890 149056 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 3 1 5 2.7 O=S(=O)(c1ccccc1F)N1CC2(CCC2)Oc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL394691 149056 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 3 1 5 2.7 O=S(=O)(c1ccccc1F)N1CC2(CCC2)Oc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
6918648 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 101089 1 None 323 14 Human 9.2 pKi = 9.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
118181453 190956 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5194574 190956 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 455 5 1 6 3.9 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
276 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
5312149 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
CHEMBL431298 3457 45 None 81 13 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.03.077
70245924 81941 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172193 81941 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
68115709 131224 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 3 1 4 4.6 C=C(C)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692965 131224 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 3 1 4 4.6 C=C(C)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
70245924 81941 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172193 81941 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
118173790 191388 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5201308 191388 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 419 4 1 6 3.3 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Cl)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
46830134 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmc.2013.05.040
CHEMBL1092241 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmc.2013.05.040
57403057 70427 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70427 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
58258868 128487 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 3 0 5 3.7 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669686 128487 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 3 0 5 3.7 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1C nan
46830134 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1092241 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
118654354 189419 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5171470 189419 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
46830134 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1092241 8133 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 373 3 0 6 3.5 CSc1nn2c(C)c3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
57403057 70427 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70427 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44476514 81936 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172187 81936 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
44476514 81936 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172187 81936 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 371 3 1 7 1.9 CNc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
58258810 128478 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669677 128478 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
68115710 131240 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692981 131240 0 None - 1 Human 9.2 pKi = 9.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
3241 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
6918649 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
CHEMBL1210710 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/jm5003952
6918836 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
CHEMBL175835 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmc.2009.08.006
9910619 176343 7 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1021/jm030030n
CHEMBL46187 176343 7 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 431 3 0 5 4.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCC4C3)cc21 10.1021/jm030030n
16118795 59780 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642851 59780 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739215 59780 0 None 954 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
3241 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918649 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
CHEMBL1210710 3465 17 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1021/acs.jmedchem.1c00224
6918836 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmcl.2007.09.016
CHEMBL175835 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1016/j.bmcl.2007.09.016
44433196 88294 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236104 88294 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 2 8 2.5 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44433198 146580 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392746 146580 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 451 4 1 8 3.2 CCN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
6918836 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
CHEMBL175835 60217 15 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 427 6 2 3 4.9 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc12 10.1021/jm8009469
9979611 16483 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 1 8 3.2 O=S(=O)(c1cn(C2CCCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
CHEMBL1242425 16483 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 1 8 3.2 O=S(=O)(c1cn(C2CCCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
52945783 16489 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 449 4 0 8 3.9 CCN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242518 16489 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 449 4 0 8 3.9 CCN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258787 127433 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 5 5.4 Cn1c2c(c3cc(S(=O)(=O)c4cn(Cc5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664780 127433 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 5 5.4 Cn1c2c(c3cc(S(=O)(=O)c4cn(Cc5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127408 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127408 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258808 127440 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL3664787 127440 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
3241 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
6918649 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
CHEMBL1210710 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.ejmech.2017.04.033
11393666 192384 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192384 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192384 0 None -1 19 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT6 receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
57394333 70428 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70428 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
57394333 70428 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70428 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
68115659 131242 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2ccc(C(C)(C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692983 131242 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 4 2 6 3.1 COc1cc(S(=O)(=O)c2ccc(C(C)(C)O)cc2)cc2c3c(oc12)CCNC3 nan
58258758 128444 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128444 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
53303985 111201 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286585 111201 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
68115702 131235 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692976 131235 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 3 1 5 3.1 COc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
53303985 111201 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286585 111201 0 None 316 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1cccc(F)c1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
58258757 128474 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669673 128474 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
68115637 131168 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1Cl nan
CHEMBL3692909 131168 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1Cl nan
3241 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
6918649 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
CHEMBL1210710 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometryDisplacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2011.06.090
196129 67456 12 None 1 15 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67456 12 None 1 15 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
10172764 110205 7 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL3260313 110205 7 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5201619 110205 7 None -2 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human recombinant 5-HT6 receptor assessed as inhibition constantBinding affinity to human recombinant 5-HT6 receptor assessed as inhibition constant
ChEMBL 385 3 0 5 3.0 CN1CCN(c2cccc3cc(S(=O)(=O)c4cccc(F)c4)cnc23)CC1 10.1021/acs.jmedchem.2c00633
57414524 131175 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692916 131175 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
44369415 43718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 401 4 1 5 2.6 COc1ccc(S(=O)(=O)N2c3ccccc3CC2(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL151295 43718 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 401 4 1 5 2.6 COc1ccc(S(=O)(=O)N2c3ccccc3CC2(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354548 44322 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.6 COc1ccc(S(=O)(=O)N2CCCc3c(Cl)cc(Cl)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL151998 44322 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.6 COc1ccc(S(=O)(=O)N2CCCc3c(Cl)cc(Cl)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940101 46635 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(I)ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154089 46635 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(I)ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10837078 201134 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 445 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2ccc3c(Cl)cccc3c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62368 201134 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 445 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2ccc3c(Cl)cccc3c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10648664 201169 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62538 201169 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
9935387 98983 0 None 158 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1021/jm050247c
CHEMBL282971 98983 0 None 158 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1021/jm050247c
9913554 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm050247c
CHEMBL29433 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm050247c
9802776 101286 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1021/jm050247c
CHEMBL299822 101286 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1021/jm050247c
18180191 165753 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCNCC1 10.1021/jm050247c
CHEMBL427155 165753 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2cccc(I)c2)cc1N1CCNCC1 10.1021/jm050247c
44398325 167711 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm050247c
CHEMBL433946 167711 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm050247c
52946846 16504 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 0 8 3.1 CN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242703 16504 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 421 3 0 8 3.1 CN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
46890218 6833 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 391 6 1 4 2.8 COCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084358 6833 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 391 6 1 4 2.8 COCC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889325 6936 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 308 3 1 5 2.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cncs3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084793 6936 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 308 3 1 5 2.4 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cncs3)ccc21 10.1016/j.bmcl.2010.03.110
11503175 153039 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 443 3 1 5 3.5 O=S(=O)(c1cccc2ccccc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL398036 153039 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 443 3 1 5 3.5 O=S(=O)(c1cccc2ccccc12)N1CCOc2c(N3CCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
9935387 98983 0 None 158 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 98983 0 None 158 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=9
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
3241 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
6918649 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
CHEMBL1210710 3465 17 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 10.1016/j.bmc.2013.05.040
9913554 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm5003952
CHEMBL29433 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm5003952
58258769 128479 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 128479 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
23757270 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
CHEMBL94093 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
16037746 77884 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 332 4 1 6 2.5 COc1cc(OC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
CHEMBL210733 77884 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 332 4 1 6 2.5 COc1cc(OC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
9913554 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm030030n
CHEMBL29433 100523 0 None 125 14 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1021/jm030030n
23757270 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
23757270 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL94093 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL94093 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
23757270 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL94093 205702 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 343 5 1 5 2.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
16117283 59832 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1642883 59832 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
CHEMBL1739658 59832 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 3 5 2.9 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)c1 10.1016/j.bmc.2010.10.033
44433194 146069 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392318 146069 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 1 8 2.5 CN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9802776 101286 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL299822 101286 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 430 3 0 4 5.4 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
276 3457 45 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
5312149 3457 45 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
CHEMBL431298 3457 45 None 81 13 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm049615n
10157412 130177 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 2 3 4.2 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL368390 130177 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 2 3 4.2 CN(C)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
68115671 131257 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 385 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)COC3)cc2c3c(oc12)CCNC3 nan
CHEMBL3692998 131257 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 385 3 1 6 3.0 COc1cc(S(=O)(=O)c2ccc3c(c2)COC3)cc2c3c(oc12)CCNC3 nan
57403058 70431 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
CHEMBL1950777 70431 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 nan
57403058 70431 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 10.1016/j.bmcl.2012.01.022
CHEMBL1950777 70431 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 405 2 1 5 3.9 Cn1cc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc21 10.1016/j.bmcl.2012.01.022
44476607 81940 2 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172192 81940 2 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acs.jmedchem.6b01662
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003952
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmcl.2021.128275
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2017.12.053
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116950
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.bmc.2022.116917
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
21071390 1956 48 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
8689 1956 48 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
CHEMBL3286580 1956 48 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
DB11957 1956 48 None 2 7 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptorDisplacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/acsmedchemlett.6b00056
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1021/jm5003759
118173771 191398 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5201491 191398 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 403 4 1 6 2.7 COc1ccc(S(=O)(=O)n2cc(C)c3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
57403057 70427 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70427 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
58258763 128490 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669689 128490 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 439 3 1 6 3.9 COc1cc(S(=O)(=O)n2ccc3ccc(F)cc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258788 128491 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669690 128491 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
46889472 6811 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 383 3 1 7 1.5 O=S(=O)(c1ccccc1)c1cnn2c(N3CCNCC3)c3c(nc12)CCC3 10.1021/jm100350r
CHEMBL1084244 6811 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 383 3 1 7 1.5 O=S(=O)(c1ccccc1)c1cnn2c(N3CCNCC3)c3c(nc12)CCC3 10.1021/jm100350r
57403057 70427 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70427 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
58258755 128475 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669674 128475 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(Cl)cc54)ccc31)C1CCC(C2)N1 nan
118173750 190197 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5183606 190197 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 463 4 1 6 3.4 COc1ccc(S(=O)(=O)n2cc(C)c3cc(Br)ccc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
68115873 131730 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 397 3 1 5 3.8 O=S(=O)(c1ccccc1)c1cc(OC(F)(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696965 131730 0 None - 1 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 397 3 1 5 3.8 O=S(=O)(c1ccccc1)c1cc(OC(F)(F)F)c2oc3c(c2c1)CNCC3 nan
44435621 88356 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236336 88356 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
118712409 113681 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 379 5 1 6 2.5 COc1cc(Cn2c(=O)ccc3cccc(OC)c32)cc(N2CCNCC2)c1 10.1021/jm5003952
CHEMBL3329450 113681 0 None - 1 Human 9.1 pKi = 9.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 379 5 1 6 2.5 COc1cc(Cn2c(=O)ccc3cccc(OC)c32)cc(N2CCNCC2)c1 10.1021/jm5003952
11326086 12658 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1187925 12658 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL534472 12658 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 367 3 2 5 2.7 Nc1ccc(S(=O)(=O)c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
10319296 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.05.076
CHEMBL443796 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.05.076
10319296 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00453-4
CHEMBL443796 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00453-4
10319296 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm030030n
CHEMBL443796 169135 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/jm030030n
44435621 88356 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236336 88356 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 0 5 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45484333 195141 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565724 195141 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 409 5 0 8 2.8 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
45484340 195151 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565746 195151 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 395 5 1 8 2.5 CNCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2cccnc21 10.1016/j.bmc.2009.05.055
49836620 18467 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276925 18467 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
4106 2466 16 None -1 33 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
5358812 2466 16 None -1 33 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
89 2466 16 None -1 33 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
CHEMBL93240 2466 16 None -1 33 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2018.04.059
58258810 128478 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669677 128478 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 2 5 3.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)cc(O)c31)C1CCC(C2)N1 nan
70301391 113677 0 None - 1 Human 9.0 pKi = 9.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 312 4 1 2 4.5 CN1CCCC1Cc1c[nH]c2ccc(OC3CCCCC3)cc12 10.1021/jm5003952
CHEMBL3329446 113677 0 None - 1 Human 9.0 pKi = 9.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 312 4 1 2 4.5 CN1CCCC1Cc1c[nH]c2ccc(OC3CCCCC3)cc12 10.1021/jm5003952
4106 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
5358812 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
89 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
CHEMBL93240 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.1c00497
1043 1552 13 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1552 13 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1552 13 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1552 13 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1552 13 None -23 28 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
58258764 127417 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127417 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258836 127421 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127421 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
4106 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
5358812 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
89 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
CHEMBL93240 2466 16 None -1 33 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2020.112149
168298034 192136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassayDisplacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassay
ChEMBL 445 6 2 6 3.2 COc1cc(NS(=O)(=O)c2ccc(OC)c(N3CCNCC3)c2)c(Cl)cc1Cl 10.1016/j.bmcl.2021.128275
CHEMBL5220473 192136 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassayDisplacement of [125I]cAMP-tracer from 5-HT6R in human HeLa cells assessed as measuring cAMP level incubated for 15 mins by radioimmunoassay
ChEMBL 445 6 2 6 3.2 COc1cc(NS(=O)(=O)c2ccc(OC)c(N3CCNCC3)c2)c(Cl)cc1Cl 10.1016/j.bmcl.2021.128275
58258798 128485 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669684 128485 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
9931929 63133 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
CHEMBL179814 63133 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 3 0 4 4.9 CN1CC=C(c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(F)cc23)CC1 10.1021/jm5003952
6918689 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
CHEMBL23038 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm5003952
118712405 113663 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 4 0 5 4.0 CN1CCC(c2cn(C)c3cc(OS(=O)(=O)c4c(F)cccc4F)ccc23)CC1 10.1021/jm5003952
CHEMBL3329432 113663 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 420 4 0 5 4.0 CN1CCC(c2cn(C)c3cc(OS(=O)(=O)c4c(F)cccc4F)ccc23)CC1 10.1021/jm5003952
11164580 113671 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 4 2 4 3.3 O=S(=O)(Nc1ccc2c(c1)C(C1CCNCC1)=CCO2)c1ccccc1 10.1021/jm5003952
CHEMBL3329440 113671 0 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 4 2 4 3.3 O=S(=O)(Nc1ccc2c(c1)C(C1CCNCC1)=CCO2)c1ccccc1 10.1021/jm5003952
59017478 113680 3 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 349 4 1 5 3.8 COc1cc(N2CCNCC2)c2ncc(C)c(Oc3ccccc3)c2c1 10.1021/jm5003952
CHEMBL3329449 113680 3 None - 1 Human 9.0 pKi = 9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 349 4 1 5 3.8 COc1cc(N2CCNCC2)c2ncc(C)c(Oc3ccccc3)c2c1 10.1021/jm5003952
58258772 127422 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127422 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258822 128480 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669679 128480 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
58258817 128486 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
CHEMBL3669685 128486 0 None - 1 Human 9.0 pKi = 9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 430 3 0 5 4.4 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1C nan
276 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
5312149 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
CHEMBL431298 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.01.031
44388943 62960 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL179277 62960 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 371 3 2 5 3.0 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44389016 63589 0 None 741 3 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180606 63589 0 None 741 3 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44389015 121816 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359876 121816 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44389004 122610 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL361180 122610 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 397 3 2 7 2.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc4c(cc32)OCO4)cc1 10.1016/j.bmcl.2004.10.064
10346043 46856 0 None 1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154274 46856 0 None 1 3 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 503 5 2 5 3.4 COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940224 47358 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 389 6 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccccc2C(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154675 47358 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 389 6 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccccc2C(C)C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9891618 106640 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 106640 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 106924 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 106924 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
9890119 206317 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 206317 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
10505579 100113 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 501 5 1 5 3.2 COc1ccc(NS(=O)(=O)c2cc(I)ccc2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL291618 100113 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 501 5 1 5 3.2 COc1ccc(NS(=O)(=O)c2cc(I)ccc2C)cc1N1CCN(C)CC1 10.1021/jm980532e
276 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
5312149 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
CHEMBL431298 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm050247c
44398570 134660 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 392 4 2 4 3.7 O=S(=O)(Oc1ccc2[nH]cc(C3CCNCC3)c2c1)c1c(F)cccc1F 10.1021/jm050247c
CHEMBL372006 134660 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 392 4 2 4 3.7 O=S(=O)(Oc1ccc2[nH]cc(C3CCNCC3)c2c1)c1c(F)cccc1F 10.1021/jm050247c
23625763 16495 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 367 3 1 6 3.1 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL1242614 16495 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 367 3 1 6 3.1 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
52946845 16503 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 407 3 1 8 2.8 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
CHEMBL1242702 16503 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 407 3 1 8 2.8 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1c(Cl)nc2sccn12 10.1016/j.ejmech.2010.05.045
71459954 78772 0 None 9 7 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
CHEMBL2113386 78772 0 None 9 7 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1016/j.bmc.2009.08.006
10136837 165410 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
CHEMBL425196 165410 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmc.2009.08.006
10154392 132993 8 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
CHEMBL370779 132993 8 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.ejmech.2017.12.053
9891618 106640 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 106640 0 None 251 6 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 106924 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 106924 0 None 251 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
9890119 206317 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 206317 0 None 158 7 Human 9.0 pKi = 9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
276 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
5312149 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
CHEMBL431298 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm030030n
6918689 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
CHEMBL23038 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1021/jm021085c
137646045 157247 0 None 436 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 404 4 0 5 4.3 CN(C)CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4083059 157247 0 None 436 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 404 4 0 5 4.3 CN(C)CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
16117151 59771 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 59771 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 59771 0 None 154 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16117279 59820 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 59820 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 59820 0 None 851 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
4106 2466 16 None -1 33 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
5358812 2466 16 None -1 33 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
89 2466 16 None -1 33 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
CHEMBL93240 2466 16 None -1 33 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jmedchem.7b00839
10108884 180483 0 None 30 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4759730 180483 0 None 30 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
134147097 149295 0 None 251 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3cccc4ccccc34)c21 10.1016/j.bmc.2016.10.010
CHEMBL3948819 149295 0 None 251 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3cccc4ccccc34)c21 10.1016/j.bmc.2016.10.010
134156091 150861 0 None 794 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2cc3ccn(S(=O)(=O)c4cccc5ccccc45)c3cc21 10.1016/j.bmc.2016.10.010
CHEMBL3961596 150861 0 None 794 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 376 4 1 4 3.9 CNCC1Cc2cc3ccn(S(=O)(=O)c4cccc5ccccc45)c3cc21 10.1016/j.bmc.2016.10.010
164619537 184973 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4863218 184973 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113783
162656068 180234 0 None 288 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756814 180234 0 None 288 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 405 4 1 7 2.3 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
126720397 180513 0 None 467 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760105 180513 0 None 467 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 389 4 1 7 1.8 CCc1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
162657540 180541 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 403 4 1 7 2.3 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4760545 180541 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 403 4 1 7 2.3 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(F)c1 10.1021/acs.jmedchem.0c02009
46889349 7003 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085036 7003 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 2 4 2.4 CNC(=O)CNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890266 7343 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 6 2 4 2.1 CNS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086573 7343 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 6 2 4 2.1 CNS(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10115854 69256 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193450 69256 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 3 0 4 3.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(I)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10291754 70091 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL194590 70091 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 3 1 5 2.9 CN1CCC(c2cn(S(=O)(=O)c3ccc(N)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
9842551 126702 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365774 126702 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 0 4 4.0 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10274389 132901 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370507 132901 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 431 5 1 5 4.5 Nc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
9902533 133079 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133079 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10136837 165410 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL425196 165410 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 3 0 4 4.1 CN1CCC(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
44433193 88293 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236103 88293 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 2 8 2.1 O=S(=O)(C1=C(Cl)NC2SC=CN12)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435625 148466 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL394233 148466 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 4 1 6 3.3 O=S(=O)(Cc1ccc(Cl)s1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44403297 132487 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL370209 132487 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccn1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
10201610 133054 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371176 133054 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10154392 132993 8 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.08.059
CHEMBL370779 132993 8 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.08.059
23655465 88958 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL236987 88958 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 2 5 2.0 NCCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm070521y
11772625 81603 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepinDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepin
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165519 81603 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepinDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter in presence of methiothepin
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2C1 10.1016/j.bmcl.2012.06.002
276 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 3457 45 None 81 13 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
6918689 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL23038 85557 3 None 812 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 381 3 1 5 2.9 Nc1ccc(S(=O)(=O)c2cc(Br)nc(N3CCCC3)c2)cc1 10.1016/j.bmcl.2007.11.045
10407367 195118 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565552 195118 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 379 5 0 5 3.6 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
10449488 195191 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565976 195191 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 333 5 1 5 2.2 CNCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836616 18615 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278179 18615 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm1007825
135804742 196358 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 5 5 4 2.2 C/C(=N\NC(=N)N)c1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm900796p
CHEMBL573982 196358 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 5 5 4 2.2 C/C(=N\NC(=N)N)c1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm900796p
136123549 196860 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 400 6 5 5 2.2 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(/C(C)=N/NC(=N)N)c3c2)cc1 10.1021/jm900796p
CHEMBL578023 196860 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 400 6 5 5 2.2 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(/C(C)=N/NC(=N)N)c3c2)cc1 10.1021/jm900796p
71151588 117755 0 None -10 10 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 117755 0 None -10 10 Human 9.0 pKi = 9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
10162467 123149 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 4 2 4 6.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL362063 123149 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 4 2 4 6.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
10182228 131927 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 9 2 3 5.5 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
CHEMBL369759 131927 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 9 2 3 5.5 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)cc12 10.1021/jm049615n
71459954 78772 0 None 9 7 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 78772 0 None 9 7 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
11314681 200044 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
CHEMBL606546 200044 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
11200511 200045 0 None 15 8 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 200045 0 None 15 8 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
11453792 200046 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606548 200046 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
11385064 200049 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606557 200049 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
11211722 200050 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606558 200050 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11246907 200064 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606636 200064 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11486933 200065 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606637 200065 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
11419238 200066 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606638 200066 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
11316095 200103 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
CHEMBL606817 200103 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 419 5 2 3 4.8 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049243i
11234629 200527 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL609741 200527 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 5 2 5 3.2 Cc1noc(C)c1S(=O)(=O)Nc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm049243i
11749539 200555 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
CHEMBL609992 200555 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3F)cc12 10.1021/jm049243i
11280663 200558 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
CHEMBL609995 200558 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 387 5 2 3 3.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3)cc12 10.1021/jm049243i
11260183 200559 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 481 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(I)cc1 10.1021/jm049243i
CHEMBL609996 200559 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 481 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(I)cc1 10.1021/jm049243i
11474995 200607 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 397 6 3 3 4.4 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
CHEMBL610253 200607 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 397 6 3 3 4.4 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
11451904 200608 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL610254 200608 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 383 5 2 3 3.9 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
68108804 131167 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131167 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
57414530 131184 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 0 4 3.9 CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692925 131184 0 None - 1 Human 9.0 pKi = 9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 0 4 3.9 CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
58258786 127403 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127403 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
58258778 127405 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664751 127405 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccc(F)cc54)ccc31)C1CCC(C2)N1 nan
16118923 59830 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642866 59830 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739656 59830 0 None 30 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
118654365 191236 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5198847 191236 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
49836618 18456 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
CHEMBL1276838 18456 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1cccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)c1 10.1021/jm1007825
10430623 18488 22 None 213 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1277105 18488 22 None 213 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
68115674 131260 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3693001 131260 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 3.9 Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
68115749 131747 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 131747 0 None - 1 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
162674158 182421 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4793608 182421 0 None -2 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
150 2473 18 None -2 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2473 18 None -2 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2473 18 None -2 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2473 18 None -2 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2473 18 None -2 15 Human 8.9 pKi = 8.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
9948345 79648 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm5003952
CHEMBL212995 79648 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm5003952
118712407 113665 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 404 4 1 9 1.4 CSc1nn2c(N3CCNCC3)nc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL3329434 113665 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 404 4 1 9 1.4 CSc1nn2c(N3CCNCC3)nc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/jm5003952
11371056 113667 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 334 5 0 5 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2sccc12 10.1021/jm5003952
CHEMBL3329436 113667 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 334 5 0 5 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2sccc12 10.1021/jm5003952
11983287 113670 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 416 6 2 6 3.7 COc1ccc(C)cc1S(=O)(=O)Nc1cc(OC2CCNCC2)c2occc2c1 10.1021/jm5003952
CHEMBL3329439 113670 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 416 6 2 6 3.7 COc1ccc(C)cc1S(=O)(=O)Nc1cc(OC2CCNCC2)c2occc2c1 10.1021/jm5003952
57403057 70427 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL1950773 70427 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 nan
57394333 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258852 127431 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5[nH]ccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664778 127431 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5[nH]ccc45)ccc31)C1CCC(C2)N1 nan
58258767 128454 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 4 5.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1Cc1ccccc1 nan
CHEMBL3669653 128454 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 481 4 1 4 5.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1Cc1ccccc1 nan
58258875 128455 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1CCO nan
CHEMBL3669654 128455 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5[nH]ccc5c4)ccc31)C1CCC(C2)N1CCO nan
58258807 128466 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1cn(S(=O)(=O)c2cc(OC)c3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3669665 128466 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1cn(S(=O)(=O)c2cc(OC)c3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258853 128476 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669675 128476 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
1346 83 108 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
280 83 108 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
9899402 83 108 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
CHEMBL9666 83 108 None 40 9 Human 8.9 pKi = 8.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1016/j.bmcl.2005.01.031
42631003 197937 10 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
CHEMBL592752 197937 10 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/acs.jmedchem.7b01898
42631003 197937 10 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
CHEMBL592752 197937 10 None -10 8 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.ejmech.2022.114464
9948345 79648 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm060469q
CHEMBL212995 79648 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1cccc(N2CCNCC2)c1 10.1021/jm060469q
44435650 88082 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235118 88082 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57403057 70427 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950773 70427 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 1 5 3.7 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccccc54)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57394333 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263299 191520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL520343 191520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 2 6 3.0 CNCCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
44474629 13965 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL1197581 13965 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
CHEMBL577570 13965 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm900796p
57414656 131185 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 3 0 4 4.3 CCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692926 131185 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 3 0 4 4.3 CCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
57414660 131191 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692932 131191 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 1 5 3.6 COc1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
68115810 131214 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 419 4 1 5 4.0 CC(C)(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692955 131214 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 419 4 1 5 4.0 CC(C)(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
68115719 131241 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692982 131241 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2cccc([C@H](C)O)c2)cc2c3c(oc12)CCNC3 nan
68115680 131715 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.5 Cc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696950 131715 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 395 2 1 4 4.5 Cc1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)cc2c3c(oc12)CCNC3 nan
44435650 88082 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235118 88082 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 381 3 1 6 3.5 O=S(=O)(c1ccc(Cl)s1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(01)00558-3
17940113 46854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 6 2.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL154273 46854 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 411 6 2 6 2.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
18354589 46966 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2cccc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154367 46966 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2cccc(Br)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940199 50012 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 421 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157173 50012 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 421 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cccc(Cl)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940155 119364 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 381 5 2 5 2.6 COc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL348870 119364 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 381 5 2 5 2.6 COc1ccc(S(=O)(=O)Nc2cccc(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918578 205942 1 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 430 4 2 5 3.7 Cc1cc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)c(C)cc1Cl 10.1016/s0960-894x(01)00558-3
CHEMBL95388 205942 1 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 430 4 2 5 3.7 Cc1cc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)c(C)cc1Cl 10.1016/s0960-894x(01)00558-3
9805456 206012 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 206012 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891617 206243 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
CHEMBL97211 206243 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
9870053 206543 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 206543 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
10528182 200953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2c(C)sc3ccc(Cl)cc23)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL61318 200953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2c(C)sc3ccc(Cl)cc23)cc1N1CCN(C)CC1 10.1021/jm980532e
136046098 67022 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 2 5 3.4 COc1cccc(-c2noc(-c3[nH]c4ccccc4c3CCN)n2)c1 10.1021/jm050247c
CHEMBL188600 67022 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 2 5 3.4 COc1cccc(-c2noc(-c3[nH]c4ccccc4c3CCN)n2)c1 10.1021/jm050247c
9867263 161882 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1021/jm050247c
CHEMBL416638 161882 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1021/jm050247c
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2010.12.007
9805456 206012 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 206012 0 None 316 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891617 206243 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
CHEMBL97211 206243 0 None 251 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
9870053 206543 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 206543 0 None 1000 4 Human 8.9 pKi = 8.9 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
46889329 7267 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 1 4 2.5 CN(CC(N)=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086253 7267 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 6 1 4 2.5 CN(CC(N)=O)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889352 7310 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 441 8 2 5 2.9 O=S(=O)(O)CCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086476 7310 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 441 8 2 5 2.9 O=S(=O)(O)CCCNC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2005.06.107
10156556 71685 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 5 2.7 O=S(=O)(c1ccccc1)c1coc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
CHEMBL197574 71685 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 1 5 2.7 O=S(=O)(c1ccccc1)c1coc2c(N3CCNCC3)cccc12 10.1016/j.bmcl.2005.06.107
11689373 93034 2 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246078 93034 2 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1ccccc1F)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44441237 93238 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 392 3 2 6 1.4 Nc1ccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cc(F)cc32)cc1 10.1016/j.bmcl.2006.12.093
CHEMBL246917 93238 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 392 3 2 6 1.4 Nc1ccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cc(F)cc32)cc1 10.1016/j.bmcl.2006.12.093
44425701 85878 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 372 6 1 3 3.9 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL231334 85878 0 None 1 5 Human 8.9 pKi = 8.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 372 6 1 3 3.9 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
44435610 88367 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236404 88367 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435629 148162 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL393997 148162 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435613 153869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL398809 153869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
16071605 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
7356 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
CHEMBL2103880 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
DB12229 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/acs.jmedchem.6b01662
16071605 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
7356 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
CHEMBL2103880 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
DB12229 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1021/jm5003952
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003952
57394333 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL1950774 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 nan
58258790 128465 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 3 1 7 3.1 COc1cc(S(=O)(=O)n2ncc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669664 128465 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 422 3 1 7 3.1 COc1cc(S(=O)(=O)n2ncc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258821 128488 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669687 128488 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 4.0 COc1cc(S(=O)(=O)n2cc(C)c3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
10047631 203163 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL75734 203163 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)c1 10.1016/s0960-894x(00)00453-4
135437144 111845 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm010943m
CHEMBL329329 111845 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm010943m
16071605 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
7356 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
CHEMBL2103880 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
DB12229 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C 10.1016/j.bmcl.2021.128275
135437144 111845 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm030030n
CHEMBL329329 111845 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 376 7 1 5 3.9 COc1cccc(Cc2noc(-c3[nH]c4ccccc4c3CCN(C)C)n2)c1 10.1021/jm030030n
118181459 189448 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 389 4 1 6 2.4 COc1ccc(S(=O)(=O)n2ccc3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5171917 189448 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 389 4 1 6 2.4 COc1ccc(S(=O)(=O)n2ccc3ccc(F)cc32)cc1N1CCNCC1 10.1016/j.bmc.2022.116917
168280735 190476 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 451 5 2 6 4.1 COc1cc(NS(=O)(=O)c2sc3cc(Cl)ccc3c2C)ccc1N1CCNCC1 10.1016/j.bmc.2022.116917
CHEMBL5187416 190476 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
ChEMBL 451 5 2 6 4.1 COc1cc(NS(=O)(=O)c2sc3cc(Cl)ccc3c2C)ccc1N1CCNCC1 10.1016/j.bmc.2022.116917
118879893 160656 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4080401 160656 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117763 160656 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
44435610 88367 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236404 88367 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435629 148162 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393997 148162 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435613 153869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398809 153869 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 1 5 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880708 7365 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1086719 7365 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 374 3 0 4 4.0 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
57394333 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950774 70428 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4c[nH]c5ccccc45)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(00)00320-6
9867263 161882 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL416638 161882 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 428 3 0 4 5.3 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3=CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2009.04.108
25263302 191387 0 None 134 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191387 0 None 134 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
25263303 183602 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 282 4 1 3 3.0 Cc1c(OCc2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483148 183602 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 282 4 1 3 3.0 Cc1c(OCc2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
68115638 131176 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692917 131176 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
68115676 131714 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696949 131714 0 None - 1 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
44388701 122619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL361213 122619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1021/jm5003952
52913108 70417 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70417 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
58258809 127394 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664740 127394 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccccc45)ccc31)C1CCC(C2)N1 nan
58258792 127408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
CHEMBL3664754 127408 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cn(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c2ccccc12 nan
58258812 128453 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 5 4.2 COCCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669652 128453 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 5 4.2 COCCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258818 128464 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 488 6 1 6 4.9 COc1cc(S(=O)(=O)c2cccc(OCc3ccccc3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669663 128464 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 488 6 1 6 4.9 COc1cc(S(=O)(=O)c2cccc(OCc3ccccc3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44388701 122619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1016/j.bmcl.2012.06.002
CHEMBL361213 122619 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 388 4 0 4 4.2 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc12 10.1016/j.bmcl.2012.06.002
9863836 205890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1021/jm030030n
CHEMBL95136 205890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1021/jm030030n
53318109 59787 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642849 59787 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739254 59787 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 5 3 5 3.3 CC(N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
11256720 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
9444 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
CHEMBL1083390 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
DB12680 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.1c00224
3052776 204830 87 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1016/j.ejmech.2020.112765
CHEMBL887 204830 87 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 171 2 1 1 1.9 C#CCN[C@@H]1CCc2ccccc21 10.1016/j.ejmech.2020.112765
11256720 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
9444 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL1083390 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
DB12680 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.ejmech.2017.12.053
11256720 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
9444 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL1083390 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
DB12680 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1021/acs.jmedchem.0c02009
44433195 146352 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392541 146352 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 1 8 2.8 CCN1CCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435616 147321 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393312 147321 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
11256720 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
9444 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
CHEMBL1083390 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
DB12680 2024 73 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 10.1016/j.bmc.2018.05.033
164619210 185081 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4864854 185081 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
9863836 205890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL95136 205890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 363 4 2 5 2.5 CNc1cc(N2CCCNCC2)ccc1S(=O)(=O)c1ccc(F)cc1 10.1016/j.bmcl.2007.11.045
49836923 18576 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277918 18576 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 5 0 6 4.4 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
52945634 16510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 4 0 8 3.5 CCN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242791 16510 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 4 0 8 3.5 CCN1CCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435616 147321 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393312 147321 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258786 127403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127403 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
24965679 83621 13 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207386 83621 13 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
10531 1392 18 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1392 18 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1392 18 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1392 18 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1392 18 None -9 24 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
9862256 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL92139 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258758 128444 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128444 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
58258757 128474 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669673 128474 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 4 4.6 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
58258838 128494 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669693 128494 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
9862256 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
9822215 205381 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
CHEMBL92093 205381 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
9862256 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL92139 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44438738 148030 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 368 4 0 4 3.9 CN(C)CC1CCCc2c1c1ccccc1n2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.12.089
CHEMBL393886 148030 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 368 4 0 4 3.9 CN(C)CC1CCCc2c1c1ccccc1n2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.12.089
16117280 59821 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642887 59821 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739614 59821 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 424 4 3 5 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
16071847 59829 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642865 59829 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739655 59829 0 None 229 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
44216882 138585 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786752 138585 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 357 4 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
44403094 134702 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 344 5 0 5 2.9 COc1ccc2c(c1)c(CN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
CHEMBL372364 134702 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 344 5 0 5 2.9 COc1ccc2c(c1)c(CN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
44435619 88355 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236335 88355 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435608 88710 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236577 88710 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880758 6018 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080729 6018 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 377 3 1 5 3.6 O=S(=O)(c1cn(C2CCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
52913108 70417 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70417 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263354 191719 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2cccc3ccccc23)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL520638 191719 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2cccc3ccccc23)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
9862256 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL92139 205391 0 None 2 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
68109269 131113 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 2 1 5 3.4 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccc(F)cc21 nan
CHEMBL3692855 131113 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 2 1 5 3.4 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)n1ccc2ccc(F)cc21 nan
68115826 131226 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 4 2 6 2.4 COc1cc(S(=O)(=O)c2ccccc2CO)cc2c3c(oc12)CCNC3 nan
CHEMBL3692967 131226 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 4 2 6 2.4 COc1cc(S(=O)(=O)c2ccccc2CO)cc2c3c(oc12)CCNC3 nan
68115682 131720 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696955 131720 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 345 2 1 4 3.4 Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
1042 1551 20 None -5 16 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1551 20 None -5 16 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1551 20 None -5 16 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1551 20 None -5 16 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1551 20 None -5 16 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
44435619 88355 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236335 88355 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435608 88710 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236577 88710 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
17940260 47848 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2ccccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155106 47848 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 5 2 5 2.7 COc1ccc(S(=O)(=O)Nc2ccccc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
17940058 50203 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 447 6 1 7 1.9 COc1ccc(S(=O)(=O)N2CCc3c(OC)ccc(OC)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157338 50203 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 447 6 1 7 1.9 COc1ccc(S(=O)(=O)N2CCc3c(OC)ccc(OC)c3C2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918579 206022 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 494 4 2 5 3.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(I)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL95878 206022 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 494 4 2 5 3.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(I)cc1 10.1016/s0960-894x(01)00558-3
9935750 206705 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 5 2 6 5.4 CC(C)c1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL99982 206705 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 5 2 6 5.4 CC(C)c1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
134137966 146889 0 None 794 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 326 4 1 4 2.7 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c21 10.1016/j.bmc.2016.10.010
CHEMBL3929918 146889 0 None 794 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 326 4 1 4 2.7 CNCC1Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c21 10.1016/j.bmc.2016.10.010
46890189 6969 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 4 1 4 3.4 COC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084874 6969 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 377 4 1 4 3.4 COC(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890191 6970 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 0 3 3.6 CC(=O)N(C)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084875 6970 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 375 4 0 3 3.6 CC(=O)N(C)C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
10177503 69477 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193665 69477 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
18180095 113921 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 477 4 1 6 4.4 Cc1c(S(=O)(=O)Nc2cc3c(c(N4CCN(C)CC4)c2)OCC3)sc2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL3331585 113921 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 477 4 1 6 4.4 Cc1c(S(=O)(=O)Nc2cc3c(c(N4CCN(C)CC4)c2)OCC3)sc2ccc(Cl)cc12 10.1021/jm5003952
58258764 127417 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127417 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258761 128477 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669676 128477 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258822 128480 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669679 128480 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)cc(O)c31)C1CCC(C2)N1 nan
9953284 203088 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.05.076
CHEMBL75010 203088 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.05.076
9953284 203088 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00453-4
CHEMBL75010 203088 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00453-4
71458811 81604 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165520 81604 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
118654427 191781 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
CHEMBL5207516 191781 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2c(N3CCNCC3)cccc21 10.1016/j.bmc.2022.116950
57396970 69400 0 None 4 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69400 0 None 4 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
11461668 62228 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 330 6 1 5 2.5 CNCCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL178254 62228 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 330 6 1 5 2.5 CNCCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.113792
71458811 81604 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
CHEMBL2165520 81604 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 2 1 4 2.3 NC1Cc2cccc3c2c(cn3S(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
11725505 197361 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585930 197361 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 351 4 1 5 3.0 NCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2cccnc21 10.1016/j.bmc.2009.05.055
9978683 18487 0 None 208 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
CHEMBL1277104 18487 0 None 208 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm1007825
44554395 18536 0 None 54 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18536 0 None 54 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
23725134 13940 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL1197475 13940 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
CHEMBL573521 13940 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 4 7 2.2 CC1Cc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc2/C1=N/NC(=N)N 10.1021/jm900796p
66801234 111609 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289995 111609 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 469 7 1 5 4.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68109281 131155 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CO)NCC3 nan
CHEMBL3692896 131155 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CO)NCC3 nan
57414792 131213 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.3 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCO)CC3 nan
CHEMBL3692954 131213 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.3 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCO)CC3 nan
68115811 131216 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 5 0 5 3.9 COCCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692957 131216 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 5 0 5 3.9 COCCN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
68115846 131733 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 5 2 6 2.3 O=S(=O)(c1ccccc1)c1cc(OCCO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696968 131733 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 5 2 6 2.3 O=S(=O)(c1ccccc1)c1cc(OCCO)c2oc3c(c2c1)CNCC3 nan
10388593 160486 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4100484 160486 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116439 160486 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
52940867 16496 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 463 4 0 8 4.3 CC(C)N1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242615 16496 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 463 4 0 8 4.3 CC(C)N1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
11961315 113656 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2c1CC[C@H](N(C)C)C2 10.1021/jm5003952
CHEMBL3329425 113656 0 None - 1 Human 8.8 pKi = 8.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.6 COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2c1CC[C@H](N(C)C)C2 10.1021/jm5003952
58258797 128483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669682 128483 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 3 1 5 4.0 COc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44397689 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL196102 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL373107 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
16019576 10796 6 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172726 10796 6 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 427 5 1 9 3.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1cccs1)c1sccc12 10.1016/j.bmc.2010.05.051
16118797 59781 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642852 59781 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739216 59781 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NC3CCCNC3)cc12 10.1016/j.bmc.2010.10.033
164613488 184437 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4854972 184437 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113783
137633076 156008 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 7 0 6 4.1 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068232 156008 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 7 0 6 4.1 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
44433199 88348 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236314 88348 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 465 4 1 8 3.6 CC(C)N1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
276 3457 45 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
5312149 3457 45 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
CHEMBL431298 3457 45 None 81 13 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.ejmech.2015.01.052
9933223 101069 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL298274 101069 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
44397689 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL196102 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL373107 71096 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
45487139 195664 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL568935 195664 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 421 6 0 6 3.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc3ccccc13)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
49836825 18535 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
CHEMBL1277564 18535 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 3 0 6 3.3 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3C)CC1 10.1021/jm1007825
49836826 18545 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277656 18545 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 0 6 3.8 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836509 18584 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277999 18584 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(F)c4)c3c2)CC1 10.1021/jm1007825
71502633 117757 0 None 64 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 533 10 0 7 5.3 CC(C)Oc1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409258 117757 0 None 64 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 533 10 0 7 5.3 CC(C)Oc1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
68109203 131133 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3692874 131133 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CCNC3 nan
68108804 131167 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131167 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
68115644 131218 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692959 131218 0 None - 1 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
162654074 179997 0 None -3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4754138 179997 0 None -3 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
12148615 113678 0 None - 1 Human 8.7 pKi = 8.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 344 4 1 4 4.1 NCCOc1cccc2c1c1cccc3c1n2[C@H](c1ccccc1)CO3 10.1021/jm5003952
CHEMBL3329447 113678 0 None - 1 Human 8.7 pKi = 8.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 344 4 1 4 4.1 NCCOc1cccc2c1c1cccc3c1n2[C@H](c1ccccc1)CO3 10.1021/jm5003952
52913104 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258764 127417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664763 127417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc(S(=O)(=O)n2ccc3ccccc32)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258758 128444 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669643 128444 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 416 2 1 5 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
58258761 128477 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669676 128477 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)cc(O)c31)C1CCC(C2)N1 nan
58258769 128479 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669678 128479 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 2 2 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)cc(O)c31)C1CCC(C2)N1 nan
44413495 77644 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
CHEMBL209724 77644 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2006.04.094
58158721 138463 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785453 138463 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 383 3 2 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(N)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
52913104 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
24776942 166142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@H]1CCCN1C 10.1021/jm070910s
CHEMBL428238 166142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@H]1CCCN1C 10.1021/jm070910s
49836827 18554 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277751 18554 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 0 6 4.2 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
49836828 18562 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
CHEMBL1277836 18562 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 4 0 6 4.4 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCN(C)CC3)ccc21 10.1021/jm1007825
25263300 184035 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484926 184035 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 1 6 3.3 CN(C)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
66801210 111632 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
CHEMBL3290017 111632 0 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 535 8 1 6 6.1 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(Cl)cc12 10.1021/jm401895u
16222549 81608 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165524 81608 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
52913104 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258786 127403 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664749 127403 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(F)ccc54)ccc31)C1CCC(C2)N1 nan
58258794 128438 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669637 128438 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
58258754 128447 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128447 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
44438722 93389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 0 4 4.0 CN(C)CCc1cn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247673 93389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 0 4 4.0 CN(C)CCc1cn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
44435652 88824 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236812 88824 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
52913104 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70415 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44405357 134968 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 3 6 2.5 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL372853 134968 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 3 6 2.5 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
44554394 18546 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277657 18546 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 4 1 6 3.5 CCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
10383646 18575 0 None 186 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277917 18575 0 None 186 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 5 2.1 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1021/jm1007825
142592130 172776 0 None 263 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4527051 172776 0 None 263 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCNCC3)c2C1 10.1016/j.bmcl.2016.07.055
11154465 60240 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
CHEMBL175940 60240 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
68109036 131120 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1ccc(Cl)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692862 131120 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1ccc(Cl)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116256 131231 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692972 131231 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 427 4 1 6 3.8 COc1cc(S(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc2c3c(oc12)CCNC3 nan
68115706 131238 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692979 131238 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
68115844 131729 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696964 131729 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(oc12)CCNC3 nan
68115747 131746 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 3 1 4 4.2 COc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696981 131746 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 3 1 4 4.2 COc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
44435652 88824 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236812 88824 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 395 3 0 6 3.9 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
16222547 81626 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165541 81626 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
44369594 48799 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 6 2 6 2.9 COc1cc(Cl)c(C)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL156130 48799 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 425 6 2 6 2.9 COc1cc(Cl)c(C)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
17940245 49954 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2ccc(I)cc2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157103 49954 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 473 5 2 5 2.5 COc1ccc(S(=O)(=O)Nc2ccc(I)cc2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10433930 50816 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157910 50816 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9957092 106728 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316643 106728 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
17940089 119158 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346990 119158 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328732 205860 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 512 4 1 6 5.5 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN5CCC[C@H]5C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL94988 205860 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 512 4 1 6 5.5 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN5CCC[C@H]5C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918577 205968 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2c(Cl)cc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL95568 205968 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2c(Cl)cc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
6918603 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9847669 206440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2c(Cl)cccc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL98353 206440 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1sc2c(Cl)cccc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
10526615 102033 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 429 5 1 5 3.6 COc1ccc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL304039 102033 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 429 5 1 5 3.6 COc1ccc(NS(=O)(=O)c2cc(Cl)cc(Cl)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
11154465 60240 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm050247c
CHEMBL175940 60240 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm050247c
6918603 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL97158 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
10320800 16488 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 3 0 8 3.5 CN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL1242517 16488 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 435 3 0 8 3.5 CN1CCCC(n2cc(S(=O)(=O)c3c(Cl)nc4sccn34)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435603 91318 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL240922 91318 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44435640 154390 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL401019 154390 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
6918603 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 206232 1 None 316 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligandBinding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
46890267 6527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 426 6 1 4 2.5 CN(C)S(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083173 6527 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 426 6 1 4 2.5 CN(C)S(=O)(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46890220 6676 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 405 5 2 4 3.0 CC(C)(O)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1083780 6676 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 405 5 2 4 3.0 CC(C)(O)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889920 7123 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 291 3 2 4 1.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cn[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1085619 7123 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 291 3 2 4 1.6 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cn[nH]c3)ccc21 10.1016/j.bmcl.2010.03.110
10273087 134279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
CHEMBL371876 134279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 375 3 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2005.06.107
22557214 93035 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1cccc(Cl)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246079 93035 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1cccc(Cl)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
20765662 93142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 398 3 1 6 1.9 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1C#N)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246500 93142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 398 3 1 6 1.9 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1C#N)CCO2 10.1016/j.bmcl.2006.12.093
42631003 197937 10 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL592752 197937 10 None -10 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
9863611 96482 0 None 7 5 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 358 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCNCC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL266018 96482 0 None 7 5 Human 8.7 pKi = 8.7 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 358 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCNCC3)cc1 10.1016/j.bmcl.2006.10.036
118712402 113657 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 306 3 1 2 4.2 Fc1ccc2c(c1)c(C1=CCNCC1)cn2Cc1ccccc1 10.1021/jm5003952
CHEMBL3329426 113657 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 306 3 1 2 4.2 Fc1ccc2c(c1)c(C1=CCNCC1)cn2Cc1ccccc1 10.1021/jm5003952
135847967 113685 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 337 3 3 4 3.4 Clc1ccc(-c2[nH]c3ccccc3c2/C=N/NC2=NCCN2)cc1 10.1021/jm5003952
CHEMBL3329454 113685 0 None - 1 Human 8.0 pKi = 8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 337 3 3 4 3.4 Clc1ccc(-c2[nH]c3ccccc3c2/C=N/NC2=NCCN2)cc1 10.1021/jm5003952
58258840 127398 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)cc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664744 127398 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)cc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258838 128494 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669693 128494 0 None - 1 Human 8.0 pKi = 8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 4 1 7 3.6 COc1cc(S(=O)(=O)c2cccc(-n3cccn3)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44389002 63233 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180066 63233 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44389001 63470 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180221 63470 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 386 3 0 4 4.3 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3Cl)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
563919 98821 4 None 1000 2 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL281937 98821 4 None 1000 2 Human 8.0 pKi = 8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 302 3 0 2 4.4 CN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
10498813 200075 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 361 5 1 5 2.2 COc1ccc(NS(=O)(=O)c2ccccc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL60669 200075 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 361 5 1 5 2.2 COc1ccc(NS(=O)(=O)c2ccccc2)cc1N1CCN(C)CC1 10.1021/jm980532e
44263491 134674 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmc.2009.08.006
CHEMBL372109 134674 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmc.2009.08.006
16718920 189085 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL515307 189085 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
46227404 198201 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
CHEMBL594548 198201 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.08.006
135398745 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
135398745 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2869 108 None -4 65 Human 8.0 pKi = 8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
135398737 944 89 None -4 91 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
38 944 89 None -4 91 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
722 944 89 None -4 91 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
CHEMBL42 944 89 None -4 91 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
DB00363 944 89 None -4 91 Human 8.0 pKi = 8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990550b
31101 720 39 None -23 35 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 720 39 None -23 35 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 720 39 None -23 35 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 720 39 None -23 35 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 720 39 None -23 35 Human 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
56945043 155864 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4066532 155864 0 None -1 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
56944956 158373 0 None -10 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4095555 158373 0 None -10 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
134155367 150683 0 None 125 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3959964 150683 0 None 125 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
90469382 185581 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4872451 185581 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.1c00224
164612723 184104 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 554 11 2 7 5.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850051 184104 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 554 11 2 7 5.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
162655699 180222 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 373 4 1 8 1.1 COc1cccc(S(=O)(=O)n2cnc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4756605 180222 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 373 4 1 8 1.1 COc1cccc(S(=O)(=O)n2cnc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
134130058 141710 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 11 0 6 5.3 CN(CCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3884709 141710 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 11 0 6 5.3 CN(CCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
134130237 141727 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 9 0 6 4.5 CN(CCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3884867 141727 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 9 0 6 4.5 CN(CCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
134130116 141740 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 565 7 1 7 5.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884988 141740 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 565 7 1 7 5.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
53310757 138604 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786973 138604 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
9969402 70203 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194750 70203 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 4 1 5 3.4 COc1ccc(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
10272846 71441 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 1 4 4.4 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196743 71441 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 1 4 4.4 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44263491 134674 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL372109 134674 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 2 1 4 2.5 Nc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1016/j.bmcl.2005.08.059
16718920 189085 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
CHEMBL515307 189085 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 422 6 1 6 3.7 CN(C)CCC1=CCc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm8009469
155528355 170769 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 424 5 2 6 3.5 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4461327 170769 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 424 5 2 6 3.5 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155533660 171335 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4469792 171335 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
155538873 172220 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4513458 172220 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155514576 175976 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4441060 175976 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4597227 175976 0 None 8 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
155515920 176110 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4442332 176110 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4598348 176110 0 None 109 4 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
23655462 89792 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL238277 89792 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1021/jm070521y
44435538 90175 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
CHEMBL238770 90175 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 338 4 2 7 1.0 CN1C=C(S(=O)(=O)n2cc(CCN)c3ccccc32)SC1N 10.1021/jm070521y
21071574 123565 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL363275 123565 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
90656165 110347 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 386 3 1 4 3.6 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260798 110347 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 386 3 1 4 3.6 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
90656170 110352 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2cccc(Cl)c2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260803 110352 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2cccc(Cl)c2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
22557257 93036 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1cccc(F)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246080 93036 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 3 1 5 1.8 O=S(=O)(c1cccc(F)c1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44425705 85653 0 None 1 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 411 4 1 5 3.8 Cc1noc(C)c1-c1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL230930 85653 0 None 1 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 411 4 1 5 3.8 Cc1noc(C)c1-c1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)cc1 10.1016/j.bmcl.2006.10.036
10217687 85804 0 None -12 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 456 5 1 4 4.8 COc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231249 85804 0 None -12 5 Human 8.0 pKi = 8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 456 5 1 4 4.8 COc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
11235953 200101 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606815 200101 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)cc12 10.1021/jm049243i
68109159 131163 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131163 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414662 131194 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 1 5 4.0 O=S(=O)(c1ccc(C2CCO2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692935 131194 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 1 5 4.0 O=S(=O)(c1ccc(C2CCO2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25263350 183789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccccc1S(=O)(=O)Oc1cccc(C2CCNCC2)c1C 10.1016/j.bmcl.2009.03.077
CHEMBL484533 183789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccccc1S(=O)(=O)Oc1cccc(C2CCNCC2)c1C 10.1016/j.bmcl.2009.03.077
11744377 156520 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4074058 156520 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
23652788 56398 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 511 3 0 5 4.2 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642423 56398 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 511 3 0 5 4.2 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
21071574 123565 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
CHEMBL363275 123565 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
10390318 155722 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(Br)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4064995 155722 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(Br)cc1 10.1021/acs.jmedchem.6b01662
24768515 126985 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/jm070521y
CHEMBL366151 126985 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/jm070521y
25263304 183603 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2cccc(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483149 183603 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2cccc(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
71449796 81636 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2F)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165551 81636 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2F)C1 10.1016/j.bmcl.2012.06.002
44403072 70066 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194568 70066 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
25263336 183753 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484337 183753 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
23652790 56395 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 465 4 0 5 3.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642420 56395 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 465 4 0 5 3.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
135398745 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
47 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
DB00334 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/acsmedchemlett.6b00482
135398745 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
47 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
DB00334 2869 108 None -4 65 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.111857
46880529 6094 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
CHEMBL1081110 6094 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 388 4 1 5 3.5 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCNC1 10.1016/j.bmcl.2010.01.073
23653062 56399 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642424 56399 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 421 4 0 5 3.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
24775948 84049 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2220110 84049 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL3216123 84049 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 1 5 2.6 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCNCC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
23652557 56389 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 389 3 0 5 3.3 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642414 56389 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 389 3 0 5 3.3 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
44435622 88671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236540 88671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162661196 180879 0 None -14 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4764468 180879 0 None -14 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
58258826 127436 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4O)ccc31)C1CCC(C2)N1 nan
CHEMBL3664783 127436 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4O)ccc31)C1CCC(C2)N1 nan
1342 36 42 None -45 18 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
3 36 42 None -45 18 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
CHEMBL277120 36 42 None -45 18 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
5 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
5202 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
CHEMBL39 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
DB08839 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2004.05.076
44401278 70744 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 277 6 1 1 4.4 CNCCC1=CC(CCc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL195317 70744 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 277 6 1 1 4.4 CNCCC1=CC(CCc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
5 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
5202 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
CHEMBL39 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
DB08839 139 66 None -169 54 Human 7.0 pKi = 7 Binding
Binding affinity to 5-Ht6 receptor (unknown origin)Binding affinity to 5-Ht6 receptor (unknown origin)
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2016.03.036
135398737 944 89 None -4 91 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 944 89 None -4 91 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 944 89 None -4 91 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 944 89 None -4 91 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 944 89 None -4 91 Human 7.0 pKi = 7 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
4106 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-5HT from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
56944861 156532 0 None -38 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4074195 156532 0 None -38 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
66801430 157172 0 None -1 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 7 2 3 4.9 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4081987 157172 0 None -1 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 7 2 3 4.9 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
137642284 157675 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4088170 157675 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccc(F)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
162672328 182411 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 538 9 1 5 5.8 C#CCNC1CCc2c(OCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4793457 182411 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 538 9 1 5 5.8 C#CCNC1CCc2c(OCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
137654042 158293 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(Cl)cccc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4094743 158293 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(Cl)cccc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
4106 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2466 16 None -7 33 Rat 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation countingDisplacement of [3H]-LSD from recombinant rat 5-Ht6 receptor expressed in HEK293 cells after 120 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
71463515 84871 3 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 1 2 1.7 CN(C)CCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260373 84871 3 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 1 2 1.7 CN(C)CCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
118732439 117884 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 427 6 1 6 3.6 CN(C)CCn1c(=O)sc2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc21 10.1016/j.ejmech.2015.01.052
CHEMBL3410504 117884 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 427 6 1 6 3.6 CN(C)CCn1c(=O)sc2cc(S(=O)(=O)Nc3cccc4ccccc34)ccc21 10.1016/j.ejmech.2015.01.052
155532983 171247 0 None 51 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 369 3 1 6 3.9 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4468396 171247 0 None 51 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 369 3 1 6 3.9 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
90656154 110336 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 340 2 1 2 3.5 O=C1CC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260786 110336 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 340 2 1 2 3.5 O=C1CC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
71152026 117740 0 None -8 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccc(F)cc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409241 117740 0 None -8 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccc(F)cc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
56944565 111557 0 None -251 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289944 111557 0 None -251 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 444 8 1 6 3.5 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
56945046 111568 0 None -16 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 7 1 6 4.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289955 111568 0 None -16 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 7 1 6 4.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
66801186 111633 0 None -30 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 457 7 1 7 3.2 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3290018 111633 0 None -30 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 457 7 1 7 3.2 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
66801246 111634 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 471 8 1 7 3.6 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3290019 111634 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 471 8 1 7 3.6 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
68115610 131104 0 None - 1 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccc(CO)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692846 131104 0 None - 1 Human 7.0 pKi = 7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccc(CO)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
11166043 61059 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL177005 61059 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
1809 134 28 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
4 134 28 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
CHEMBL18840 134 28 None -6918 36 Human 6.0 pKi = 6 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
11408954 156874 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 477 7 1 7 4.7 O=S(=O)(Nc1ccc2c(ccn2CCCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
CHEMBL407860 156874 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 477 7 1 7 4.7 O=S(=O)(Nc1ccc2c(ccn2CCCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
10708918 206357 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm050247c
CHEMBL97819 206357 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm050247c
CHEMBL5074190 212543 0 None -398 9 Human 6.0 pKi = 6 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
10708918 206357 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm030030n
CHEMBL97819 206357 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 4 4 7 0.5 CNc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(N)n1 10.1021/jm030030n
33630 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178379 94 None -13 27 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
124087 1362 106 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
7157 1362 106 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
814 1362 106 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
CHEMBL1172 1362 106 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
DB00967 1362 106 None -28 15 Human 6.0 pKi = 6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 nan
164628882 185868 0 None -5011 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 477 6 0 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3C(=O)c4ccccc4S3(=O)=O)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4876545 185868 0 None -5011 5 Human 5.0 pKi = 5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 477 6 0 6 3.4 COc1ccccc1N1CCN(Cc2ccc(CN3C(=O)c4ccccc4S3(=O)=O)cc2)CC1 10.1016/j.bmcl.2021.128028
155519393 169851 0 None 8 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 397 7 2 4 5.3 COc1ccc2[nH]cc(CCNCc3ccc(-c4cnc5ccccc5c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4448285 169851 0 None 8 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 397 7 2 4 5.3 COc1ccc2[nH]cc(CCNCc3ccc(-c4cnc5ccccc5c4)o3)c2c1 10.1016/j.ejmech.2019.111857
164619290 185223 0 None -6 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 463 7 0 5 4.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4866981 185223 0 None -6 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 463 7 0 5 4.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2021.128028
126720429 162400 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4174680 162400 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
57390799 70425 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 356 2 1 6 2.1 Cn1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)n1 10.1016/j.bmcl.2012.01.022
CHEMBL1950771 70425 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 356 2 1 6 2.1 Cn1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)n1 10.1016/j.bmcl.2012.01.022
44395458 124521 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 6 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL364351 124521 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 6 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
11522698 93675 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 325 6 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL249188 93675 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 325 6 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
137660741 158822 0 None -33 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4100470 158822 0 None -33 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
71462179 81017 0 None -7 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 406 7 1 5 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159472 81017 0 None -7 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 406 7 1 5 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
71455002 81034 0 None -51 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159489 81034 0 None -51 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
155544836 174446 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4567160 174446 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
156019563 177413 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 364 5 0 4 4.1 C=CCOc1c(OC)cc2c3c1-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4646172 177413 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 364 5 0 4 4.1 C=CCOc1c(OC)cc2c3c1-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL5073337 212521 0 None -24 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccc(Cl)cc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
137645926 157023 0 None -27 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4080398 157023 0 None -27 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
3191 102385 93 None -15 25 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -15 25 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
44456033 155027 3 None -794 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 155027 3 None -794 8 Human 6.0 pKi = 6.0 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
49799703 10890 3 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173577 10890 3 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 5 1 8 5.2 CC(Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2010.05.051
9903598 202660 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 272 4 0 3 3.1 COc1ccc2c(c1)c(CCN(C)C)c1n2CCCC1 10.1021/jm990550b
CHEMBL7172 202660 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 272 4 0 3 3.1 COc1ccc2c(c1)c(CCN(C)C)c1n2CCCC1 10.1021/jm990550b
155524491 170389 0 None -128 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccccc2Cl)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4455658 170389 0 None -128 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccccc2Cl)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155534184 171376 0 None -67 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccccc2F)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4470437 171376 0 None -67 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccccc2F)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
155514505 169281 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 1 4 5.2 COc1cccc(-c2ccc(CNC(C)Cc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4440075 169281 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 1 4 5.2 COc1cccc(-c2ccc(CNC(C)Cc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155553745 174872 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4576700 174872 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
13069622 120104 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360999 120104 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546120 120104 0 None -933 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 410 7 0 8 1.4 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
134147124 149448 0 None -19 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2ncccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3950020 149448 0 None -19 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2ncccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
58258824 127429 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)ccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664776 127429 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cc(Cl)ccn4)ccc31)C1CCC(C2)N1 nan
1342 36 42 None -45 18 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 36 42 None -45 18 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 36 42 None -45 18 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
145986138 164917 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239705 164917 0 None -6 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
137644790 157523 0 None -28 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4086211 157523 0 None -28 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
1016 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
2561 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
2733526 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
5384 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
CHEMBL83 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
DB00675 3690 75 None -38 35 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1021/jm2011657
3158 55974 21 None -851 20 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011657
CHEMBL1628227 55974 21 None -851 20 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1021/jm2011657
155532396 171229 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 399 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4468014 171229 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 399 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
57399866 71197 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949974 71197 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1962960 71197 0 None -72 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
44420568 165652 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 1 2 3.9 COc1ccc2[nH]cc(CCN(C)Cc3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
CHEMBL426567 165652 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 1 2 3.9 COc1ccc2[nH]cc(CCN(C)Cc3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
68115788 131742 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 380 3 1 7 2.5 O=S(=O)(c1ccccc1)c1cc(-n2cncn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696977 131742 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 380 3 1 7 2.5 O=S(=O)(c1ccccc1)c1cc(-n2cncn2)c2oc3c(c2c1)CNCC3 nan
164618482 185333 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4868911 185333 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
53323441 59827 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642879 59827 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739647 59827 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 3.8 O=C(NCCN1CCCCC1)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
126720442 162489 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(Cl)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176014 162489 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(Cl)cc1 10.1016/j.ejmech.2017.12.053
155548275 173217 0 None 74 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 426 5 2 5 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4537701 173217 0 None 74 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 426 5 2 5 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
11408932 60668 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 476 3 0 5 5.2 Cc1c(S(=O)(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL176258 60668 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 476 3 0 5 5.2 Cc1c(S(=O)(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)sc2ccc(Cl)cc12 10.1021/jm049615n
134137332 142476 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2ncccc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3894679 142476 0 None -33 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2ncccc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
164621422 185194 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 465 8 1 5 4.9 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4866550 185194 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 465 8 1 5 4.9 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
86288948 112129 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233679 112129 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302600 112129 0 None -3548 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 456 7 2 6 1.8 COc1ccccc1N1CCN(CC(O)CN2C(=O)NC(C)(c3ccc(F)cc3)C2=O)CC1 10.1016/j.ejmech.2014.01.065
13437718 179916 9 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 273 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2c(O)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4753238 179916 9 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 273 2 1 4 2.6 O=S(=O)(c1ccccc1)n1ccc2c(O)cccc21 10.1016/j.ejmech.2020.112916
126720395 162000 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4168165 162000 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
11601955 93849 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 306 4 1 4 2.9 CN1CCN(c2ccc(C#N)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250401 93849 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 306 4 1 4 2.9 CN1CCN(c2ccc(C#N)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
11420098 60479 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 1 5 5.7 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL176162 60479 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 1 5 5.7 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
57400828 68086 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917349 68086 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
1353 1880 85 None -1047 85 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
3559 1880 85 None -1047 85 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
86 1880 85 None -1047 85 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL54 1880 85 None -1047 85 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
DB00502 1880 85 None -1047 85 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2018.01.002
168288545 191167 0 None -239 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 372 8 3 9 1.1 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5197737 191167 0 None -239 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 372 8 3 9 1.1 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
142601328 184420 0 None -69 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4854605 184420 0 None -69 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
117209858 183971 1 None -6 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 183971 1 None -6 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
168289915 190958 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194614 190958 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 553 11 4 8 4.9 Nc1nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155511424 168978 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 7 2 3 4.8 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccccc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4435529 168978 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 7 2 3 4.8 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccccc4)o3)c12 10.1016/j.ejmech.2019.111857
135367405 163644 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4210782 163644 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 227 1 2 2 2.1 Cc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4534980 212234 15 None 2 3 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000345a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000345a HTR6
ChEMBL None None None CN(C)[C@H]1CCN(c2cc(-c3ccccc3)nc3ccnn23)C1 nan
118712406 113664 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 3.1 Cc1cc(C)cc(S(=O)(=O)c2ccc3ccnc(N4CCNCC4)c3c2)c1 10.1021/jm5003952
CHEMBL3329433 113664 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 381 3 1 5 3.1 Cc1cc(C)cc(S(=O)(=O)c2ccc3ccnc(N4CCNCC4)c3c2)c1 10.1021/jm5003952
52913224 70420 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950765 70420 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 nan
52912983 127382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc(O)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664729 127382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc(O)cc4)ccc31)C1CCC(C2)N1 nan
67085672 127392 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 2 5 4.2 CC(C)Nc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664738 127392 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 2 5 4.2 CC(C)Nc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258860 127396 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1ccccc1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
CHEMBL3664742 127396 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1ccccc1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
58258829 128450 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669649 128450 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OCc5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
9821904 19251 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1Cl 10.1021/jm010943m
CHEMBL129614 19251 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1Cl 10.1021/jm010943m
135398737 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
155523355 170181 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc2ncccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4452416 170181 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc2ncccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
155557772 174109 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4559172 174109 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
118626142 165267 0 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248491 165267 0 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
155542321 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
CHEMBL4520796 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2022.114645
163196460 192090 3 None 3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 394 4 1 7 3.4 CN1CCN(c2nc(N)nc(C(C)(C)Sc3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2022.114645
CHEMBL5219240 192090 3 None 3 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 394 4 1 7 3.4 CN1CCN(c2nc(N)nc(C(C)(C)Sc3ccc4ccccc4c3)n2)CC1 10.1016/j.ejmech.2022.114645
155542321 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4520796 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
118654519 190671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5190429 190671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 391 4 1 5 3.2 O=S(=O)(c1ccccc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
90469046 184071 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 392 3 1 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4849693 184071 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 392 3 1 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164610452 183916 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4847373 183916 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 517 11 2 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
155542321 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constant
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.bmcl.2021.128275
CHEMBL4520796 172554 0 None 38 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]LSD from 5-HT6R (unknown origin) expressed in HEK293 cells assessed as inhibition constant
ChEMBL 356 5 1 7 2.2 Cc1ccc(C(C)C)c(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.bmcl.2021.128275
44403048 132184 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL369910 132184 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 458 4 0 5 5.7 Cc1c(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
44435622 88671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236540 88671 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 355 4 0 5 3.1 CCN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
164628531 185882 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4876727 185882 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
52913224 70420 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950765 70420 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4cccc(O)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164609111 183805 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4845762 183805 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cc(Cl)cc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
164609145 183889 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4846931 183889 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
25024332 62621 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785055 62621 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C)cc3)c2)CC1 10.1021/ml100101u
44420491 83349 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c1c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.08.068
CHEMBL220566 83349 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c1c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2006.08.068
23655287 88260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
CHEMBL235985 88260 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 378 4 1 4 3.1 NCCc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1021/jm070521y
127047898 139293 0 None 56 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 440 6 0 6 3.9 CCc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
CHEMBL3798953 139293 0 None 56 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 440 6 0 6 3.9 CCc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
49836717 18494 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277192 18494 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
71151756 117758 0 None 10 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 547 11 0 7 5.6 CC(C)Oc1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409259 117758 0 None 10 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 547 11 0 7 5.6 CC(C)Oc1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
57391618 71125 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71125 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71125 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57391567 71193 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71193 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71193 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57393363 71220 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71220 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71220 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
11441064 200093 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606764 200093 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
68115755 131741 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1cc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)cn1 nan
CHEMBL3696976 131741 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1cc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)cn1 nan
58149664 126901 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
CHEMBL3659970 126901 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 408 3 1 7 2.9 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1cccc(Cl)c1)CNCC3 nan
44435633 89111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237389 89111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
24965678 83607 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207372 83607 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44435633 89111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237389 89111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 417 4 0 5 4.6 CC(C)N1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
25024528 62629 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 4 0 5 4.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cc(C(F)(F)F)ccc3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1785062 62629 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 471 4 0 5 4.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cc(C(F)(F)F)ccc3Cl)c2)CC1 10.1021/ml100101u
45487128 196110 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571878 196110 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 389 6 0 6 2.8 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1cccc(F)c1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
25263353 183550 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 359 5 1 4 3.8 CCc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL482749 183550 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 359 5 1 4 3.8 CCc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
131999484 182021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182021 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
44435631 89247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237594 89247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
137649408 156976 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4079859 156976 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44435631 89247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237594 89247 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 3 0 5 3.8 CN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
137630144 160504 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4085003 160504 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116567 160504 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44240860 138652 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787525 138652 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 388 3 3 4 1.5 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
25263307 183656 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2ccccc2F)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483559 183656 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.1 Cc1c(OCc2ccccc2F)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
45484298 195621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568673 195621 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)ccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
134131322 141676 0 None -1174 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(Cl)ccc1Cl 10.1016/j.ejmech.2016.09.008
CHEMBL3884161 141676 0 None -1174 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(Cl)ccc1Cl 10.1016/j.ejmech.2016.09.008
162663078 181412 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4780470 181412 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
23624297 56388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642413 56388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 373 3 0 5 2.8 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
56944863 156178 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4070254 156178 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
156020908 177457 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4646868 177457 0 None -2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 0 6 5.4 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
145959871 161460 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)ccnc32)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4159555 161460 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)ccnc32)cc1 10.1016/j.ejmech.2017.12.053
54582158 62205 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782359 62205 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
54586019 62207 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782361 62207 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
49836718 18495 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277193 18495 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
66801115 111572 0 None -11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 506 7 1 7 4.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289959 111572 0 None -11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 506 7 1 7 4.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68108771 131159 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1CNCc2c1oc1c(Cl)cc(S(=O)(=O)c3ccccc3)cc21 nan
CHEMBL3692900 131159 0 None - 1 Human 7.0 pKi = 7.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1CNCc2c1oc1c(Cl)cc(S(=O)(=O)c3ccccc3)cc21 nan
66801673 111582 0 None -32 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289969 111582 0 None -32 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
66801333 111596 0 None -6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 7 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289982 111596 0 None -6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 7 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
156020306 177555 0 None -26 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 602 11 0 6 6.9 O=S(=O)(c1ccccc1)N(CCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2020.115459
CHEMBL4648390 177555 0 None -26 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 602 11 0 6 6.9 O=S(=O)(c1ccccc1)N(CCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc(C(F)(F)F)c1 10.1016/j.bmc.2020.115459
2389 3279 114 None -2454 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
5073 3279 114 None -2454 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
96 3279 114 None -2454 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
CHEMBL85 3279 114 None -2454 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
DB00734 3279 114 None -2454 67 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2018.01.002
122442272 137820 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137820 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137820 0 None -3 15 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
155529153 170835 0 None 3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 378 4 1 6 0.3 CC([Se]c1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4462404 170835 0 None 3 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 378 4 1 6 0.3 CC([Se]c1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
68115782 131739 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 384 3 1 5 2.6 CN(C)C(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696974 131739 0 None - 1 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 384 3 1 5 2.6 CN(C)C(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
155561906 175195 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4583613 175195 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
2801 161325 56 None -5 28 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm2011657
CHEMBL1200710 161325 56 None -5 28 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm2011657
CHEMBL415 161325 56 None -5 28 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 10.1021/jm2011657
9947817 4978 0 None -204 9 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105261 4978 0 None -204 9 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
2286 3134 48 None -26 29 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -26 29 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -26 29 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -26 29 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -26 29 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
155561915 175896 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4585051 175896 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596544 175896 0 None -6 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2C(F)(F)F)CC1 10.1016/j.bmc.2019.06.028
162673753 182474 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 566 11 1 5 6.5 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4794139 182474 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 566 11 1 5 6.5 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
57400391 69408 0 None -6 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935598 69408 0 None -6 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
9979313 5898 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 4 4.9 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079978 5898 4 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 4 4.9 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
134130475 141791 0 None -562 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cccc(Cl)c1Cl 10.1016/j.ejmech.2016.09.008
CHEMBL3885471 141791 0 None -562 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 516 7 0 7 5.5 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cccc(Cl)c1Cl 10.1016/j.ejmech.2016.09.008
145971561 163957 0 None -29 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 444 4 1 4 3.7 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)c(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4214709 163957 0 None -29 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 444 4 1 4 3.7 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)c(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
22330705 117439 6 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 438 3 0 3 5.5 Cc1ccc(Cl)cc1N(C)C(=O)c1cn(-c2ccc(F)cc2F)c(=O)c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403345 117439 6 None 1 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 438 3 0 3 5.5 Cc1ccc(Cl)cc1N(C)C(=O)c1cn(-c2ccc(F)cc2F)c(=O)c2ccccc12 10.1016/j.bmcl.2015.03.049
168291906 191432 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 452 8 0 5 4.8 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5201984 191432 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 452 8 0 5 4.8 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
2801 161325 56 None -5 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -5 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -5 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
627240 93748 9 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 7 2 6 2.5 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL249628 93748 9 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 7 2 6 2.5 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccccc1 10.1016/j.bmcl.2007.09.016
122442272 137820 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137820 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137820 0 None -3 15 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor by radioligand binding assayBinding affinity to human 5HT6 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
156014041 176634 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4635363 176634 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2020.115459
72198191 89390 0 None -141 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
CHEMBL2377445 89390 0 None -141 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 5 2 3 4.5 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
155538236 171805 0 None -42 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4476164 171805 0 None -42 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 496 7 1 5 5.2 O=c1c(-c2ccccc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
57403056 70404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 nan
CHEMBL1950749 70404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 nan
58258849 128459 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(C#N)c31)C1CCC(C2)N1 nan
CHEMBL3669658 128459 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(C#N)c31)C1CCC(C2)N1 nan
11849796 79331 1 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 229 4 1 2 3.3 NCCc1cccc(Sc2ccccc2)c1 10.1021/jm060469q
CHEMBL211688 79331 1 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 229 4 1 2 3.3 NCCc1cccc(Sc2ccccc2)c1 10.1021/jm060469q
162653138 179819 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 314 5 0 4 3.7 CCCCS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4752004 179819 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 314 5 0 4 3.7 CCCCS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
134136134 143904 0 None -120 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 584 15 1 6 5.5 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3906408 143904 0 None -120 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 584 15 1 6 5.5 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
9904281 47485 24 None -26 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1548 47485 24 None -26 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
118626089 164921 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239823 164921 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44403086 69954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 327 2 2 5 2.1 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194360 69954 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 327 2 2 5 2.1 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
118626089 164921 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239823 164921 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6R after 120 mins by scintillation counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
68109154 131135 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692876 131135 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
11177658 60206 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
CHEMBL175794 60206 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
168279625 190413 0 None -21 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4cccc(Cl)c4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5186688 190413 0 None -21 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4cccc(Cl)c4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
118724645 120089 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361003 120089 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545907 120089 0 None -48 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 367 5 0 7 1.3 Cn1c(=O)c2c(ncn2CCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
44387817 60207 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 6 2 5 3.4 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2n1 10.1021/jm049615n
CHEMBL175798 60207 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 6 2 5 3.4 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2n1 10.1021/jm049615n
CHEMBL5080719 212930 0 None -42 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccccc3o2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
2136365 117424 21 None 3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 0 5 4.5 Cc1ccc(S(=O)(=O)c2nc(N3CCc4ccccc4C3)sc2Cl)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403331 117424 21 None 3 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 0 5 4.5 Cc1ccc(S(=O)(=O)c2nc(N3CCc4ccccc4C3)sc2Cl)cc1 10.1016/j.bmcl.2015.03.049
118712404 113659 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 335 2 2 3 4.2 O=C(Nc1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL3329428 113659 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 335 2 2 3 4.2 O=C(Nc1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
44388954 121538 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 331 2 1 3 4.4 CN1CC=C(c2cn(C(=O)Nc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL359604 121538 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 331 2 1 3 4.4 CN1CC=C(c2cn(C(=O)Nc3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
155543653 172624 0 None 4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1cccc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4522568 172624 0 None 4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1cccc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
71163244 172791 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4527388 172791 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
44401549 133036 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.5 Nc1ccc(CC2=CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL371048 133036 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.5 Nc1ccc(CC2=CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
168282819 190616 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 419 10 4 8 3.1 COc1ccccc1OCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5189520 190616 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 419 10 4 8 3.1 COc1ccccc1OCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
137653850 158499 0 None -66 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4096866 158499 0 None -66 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
1222 1634 44 None -138 32 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
3396 1634 44 None -138 32 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
85 1634 44 None -138 32 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
CHEMBL46516 1634 44 None -138 32 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
DB04842 1634 44 None -138 32 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm2011657
12005903 50950 12 None 2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2021.128275
CHEMBL1580288 50950 12 None 2 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2021.128275
197033 197473 58 None -15 8 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat recombinant 5HT6 receptorBinding affinity to rat recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 197473 58 None -15 8 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat recombinant 5HT6 receptorBinding affinity to rat recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
162665888 181716 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.7 O=S(=O)(c1ccccc1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4784080 181716 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.7 O=S(=O)(c1ccccc1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
137650127 156992 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)c(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4080086 156992 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)c(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
2891368 93607 10 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 6 1 5 3.0 CN1CCN(c2ccc([N+](=O)[O-])c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL248844 93607 10 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 6 1 5 3.0 CN1CCN(c2ccc([N+](=O)[O-])c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12005903 50950 12 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
CHEMBL1580288 50950 12 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
56593643 65349 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834335 65349 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)ccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
2389 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
5073 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
96 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
CHEMBL85 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
DB00734 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2020.127506
13069627 120101 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361001 120101 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546113 120101 0 None -239 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 444 7 0 8 2.1 Cn1c(=O)c2c(ncn2CCCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
17374371 117423 9 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 447 5 1 5 4.7 O=S(=O)(Nc1ccn(Cc2cccc3ccccc23)n1)c1ccc(Br)s1 10.1016/j.bmcl.2015.03.049
CHEMBL3403330 117423 9 None -2 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 447 5 1 5 4.7 O=S(=O)(Nc1ccn(Cc2cccc3ccccc23)n1)c1ccc(Br)s1 10.1016/j.bmcl.2015.03.049
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
11316536 200094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm5003952
CHEMBL606765 200094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm5003952
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44388931 63783 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180826 63783 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
3028955 134654 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 292 6 0 2 4.0 CN(C)CCc1cn(CCc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
CHEMBL371978 134654 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 292 6 0 2 4.0 CN(C)CCc1cn(CCc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
9799635 17837 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)c(C)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126374 17837 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)c(C)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1007/s00044-004-0121-8
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmc.2009.08.006
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
53318111 59772 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642862 59772 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739117 59772 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 380 6 3 5 2.6 NCCNCc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53323436 59816 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642870 59816 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739585 59816 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
44568061 183012 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL480123 183012 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
44568139 191986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 354 3 0 4 3.3 CCN1CCc2c(n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL521419 191986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 354 3 0 4 3.3 CCN1CCc2c(n(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
155551219 173404 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4541828 173404 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cc2ccccc2cn1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
132525570 163093 0 None -7 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
CHEMBL4204059 163093 0 None -7 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 300 5 0 5 2.8 CCCCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
118654355 190667 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5190378 190667 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
90469119 184821 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 4.1 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4861001 184821 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 4.1 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164622997 185549 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 491 14 2 6 4.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4871964 185549 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 491 14 2 6 4.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
134130472 141789 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 474 8 1 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885452 141789 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 474 8 1 6 3.8 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
137633569 155828 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4066125 155828 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
2906325 154335 11 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 5 1 5 3.5 CC(Nc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-])c1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL400704 154335 11 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 340 5 1 5 3.5 CC(Nc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-])c1ccccc1 10.1016/j.bmcl.2007.09.016
44403104 72134 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198941 72134 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 422 4 0 4 4.8 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44435637 88934 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236976 88934 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
164614828 184687 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4858771 184687 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
164624322 185554 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 422 8 1 4 3.9 Cc1cccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4872078 185554 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 422 8 1 4 3.9 Cc1cccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164629020 185720 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 470 8 1 5 5.5 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.ejmech.2021.113792
CHEMBL4874512 185720 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 470 8 1 5 5.5 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.ejmech.2021.113792
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
127045871 139508 0 None 53 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 446 5 0 7 4.0 Cc1cc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)c(C)s1 10.1016/j.bmcl.2016.04.024
CHEMBL3800251 139508 0 None 53 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 446 5 0 7 4.0 Cc1cc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)c(C)s1 10.1016/j.bmcl.2016.04.024
49836619 18457 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276839 18457 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 386 4 1 6 2.2 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
24783810 175623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459371 175623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 421 4 0 6 4.0 CCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
155550351 174551 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4569676 174551 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
57396813 71201 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None 5 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
11316536 200094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
CHEMBL606765 200094 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(C(F)(F)F)c3)cc12 10.1021/jm049243i
88597039 131119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 4 4.1 [C-]#[N+]c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692861 131119 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 4 4.1 [C-]#[N+]c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
68108726 131143 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccc(CO)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692884 131143 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1ccc(CO)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68109100 131161 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 315 2 1 3 4.9 Clc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692902 131161 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 315 2 1 3 4.9 Clc1cc(Sc2ccccc2)cc2c3c(oc12)CCNC3 nan
44435637 88934 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236976 88934 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
16222656 81628 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 456 3 0 4 5.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165543 81628 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 456 3 0 4 5.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003759
11595209 94400 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253708 94400 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2ccc(O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
25024326 62623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3F)c2)CC1 10.1021/ml100101u
CHEMBL1785057 62623 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 5 0 5 3.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3F)c2)CC1 10.1021/ml100101u
16222449 81618 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165534 81618 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2448158 81618 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
10356663 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
CHEMBL328816 111451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 2 1 4 2.8 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
132495283 148756 0 None 100 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3944687 148756 0 None 100 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
20765678 93033 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 3 1 5 1.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246077 93033 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 3 1 5 1.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
44425708 152378 0 None -3 5 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 468 5 1 3 6.0 CC(C)c1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL397476 152378 0 None -3 5 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 468 5 1 3 6.0 CC(C)c1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
275 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
3246 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
5312144 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
CHEMBL46071 3308 6 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
71151889 117752 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 502 9 1 5 5.0 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409253 117752 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 502 9 1 5 5.0 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2014.12.045
164608896 183838 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 183838 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
15391752 181748 0 None -6 7 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4784373 181748 0 None -6 7 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 411 7 1 5 4.6 CC(=O)Nc1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
1342 36 42 None -45 18 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
3 36 42 None -45 18 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
CHEMBL277120 36 42 None -45 18 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxy tryptamine 6 receptorBinding affinity against 5-hydroxy tryptamine 6 receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/j.bmcl.2005.01.031
66803497 157965 0 None -21 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4091193 157965 0 None -21 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(Cl)c1 10.1021/acs.jmedchem.7b00839
66800823 111574 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 7 1 7 4.4 Cc1c(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289961 111574 0 None -14 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 7 1 7 4.4 Cc1c(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
66801379 111579 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 8 3.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3289966 111579 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 8 3.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
10324985 76428 7 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76428 7 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76428 7 None -89 17 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
44435193 90794 0 None -7 7 Human 5.9 pKi = 5.9 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
CHEMBL240045 90794 0 None -7 7 Human 5.9 pKi = 5.9 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 331 2 0 2 5.6 CC(C(=O)N1c2ccccc2Sc2ccccc21)c1ccccc1 10.1016/j.bmcl.2013.04.082
90656156 110338 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCCNC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260788 110338 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCCNC2 10.1016/j.bmcl.2014.03.049
162648882 179301 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN(CC(F)(F)F)CC3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4745715 179301 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN(CC(F)(F)F)CC3)cc21 10.1016/j.ejmech.2020.112916
132525569 163497 0 None -16 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 272 3 0 5 2.1 CCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
CHEMBL4208934 163497 0 None -16 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr
ChEMBL 272 3 0 5 2.1 CCc1cc(-c2ccoc2)nc(N2CCN(C)CC2)n1 10.1021/acs.jmedchem.7b01898
155568794 175524 0 None -4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 336 7 3 4 3.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cn[nH]c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4591410 175524 0 None -4 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 336 7 3 4 3.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cn[nH]c4)o3)c2c1 10.1016/j.ejmech.2019.111857
13069655 120095 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3360992 120095 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546106 120095 0 None -100 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 412 6 0 9 0.7 COc1ccccc1N1CCN(CCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
24966381 83620 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207385 83620 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
10252130 6022 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080741 6022 4 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCCN(Cc3ccccc3)C2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164608823 183884 0 None -64 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 480 9 0 6 4.8 CN1CCN(Cc2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
CHEMBL4846866 183884 0 None -64 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 480 9 0 6 4.8 CN1CCN(Cc2ccc(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
2848343 93948 16 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 441 4 0 7 3.7 CN1CCN(c2ccc([N+](=O)[O-])c(-n3nc(-c4ccccc4)c4ccccc4c3=O)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250840 93948 16 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 441 4 0 7 3.7 CN1CCN(c2ccc([N+](=O)[O-])c(-n3nc(-c4ccccc4)c4ccccc4c3=O)c2)CC1 10.1016/j.bmcl.2007.09.016
118724643 120091 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361002 120091 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545933 120091 0 None -28 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 353 4 0 7 0.9 Cn1c(=O)c2c(ncn2CCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
168292191 191426 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
CHEMBL5201892 191426 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
54580394 62299 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 385 4 1 5 3.2 COc1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783606 62299 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 385 4 1 5 3.2 COc1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
68115615 131183 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 424 3 0 5 4.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(c1cccnc1)CC3 nan
CHEMBL3692924 131183 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 424 3 0 5 4.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(c1cccnc1)CC3 nan
11463924 60218 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL175836 60218 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2n1CCN(C)C 10.1021/jm049615n
2274 3124 53 None -23 32 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -23 32 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -23 32 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -23 32 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -23 32 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44568064 182433 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 5 0 5 3.7 CCCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL479375 182433 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 5 0 5 3.7 CCCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
162652278 179682 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(-c2ccncc2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4750481 179682 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(-c2ccncc2)c2ccccc21 10.1016/j.ejmech.2020.112916
49836720 18504 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
CHEMBL1277287 18504 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
68109552 131146 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2cccn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692887 131146 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2cccn2)c2oc3c(c2c1)CNCC3 nan
11442097 119991 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 442 3 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3csc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL354417 119991 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 442 3 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3csc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
1016 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -38 35 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
49836505 18553 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277750 18553 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 376 3 2 5 2.5 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
155568628 175515 0 None -21 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4591250 175515 0 None -21 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
11166261 60199 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 428 3 0 5 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2csc3ccccc23)CC1 10.1021/jm049615n
CHEMBL175732 60199 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 428 3 0 5 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2csc3ccccc23)CC1 10.1021/jm049615n
5 139 66 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
5202 139 66 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
CHEMBL39 139 66 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
DB08839 139 66 None -169 54 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
44364048 38902 0 None -63 6 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
CHEMBL146942 38902 0 None -63 6 Human 6.9 pKi = 6.9 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
134153624 151938 0 None 7 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3971039 151938 0 None 7 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
44441242 93319 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 5 3.2 CN(C)CCNc1cccc2c1OC(C)(C)CN2S(=O)(=O)c1cccc(F)c1 10.1016/j.bmcl.2006.12.093
CHEMBL247325 93319 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 5 3.2 CN(C)CCNc1cccc2c1OC(C)(C)CN2S(=O)(=O)c1cccc(F)c1 10.1016/j.bmcl.2006.12.093
145960299 161770 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 4 1 5 2.7 Clc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164639 161770 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 4 1 5 2.7 Clc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
10541285 67288 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2ccc3cc[nH]c3c2)cc1 10.1021/jm050247c
CHEMBL190468 67288 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2ccc3cc[nH]c3c2)cc1 10.1021/jm050247c
145983751 164953 0 None -251 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1ccnc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240642 164953 0 None -251 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1ccnc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
155568224 175547 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 350 4 1 7 2.2 CN1CCN(c2nc(N)nc(CSc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4591878 175547 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 350 4 1 7 2.2 CN1CCN(c2nc(N)nc(CSc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
145951217 162339 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4173628 162339 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
25263310 183525 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 283 4 1 4 2.4 Cc1c(OCc2cccnc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482573 183525 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 283 4 1 4 2.4 Cc1c(OCc2cccnc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
2389 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
5073 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
96 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
CHEMBL85 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
DB00734 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/acs.jmedchem.8b01096
2389 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
5073 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
96 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
CHEMBL85 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
DB00734 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2016.09.008
2775690 92579 47 None -47 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 92579 47 None -47 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
118626169 165023 0 None -177 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242268 165023 0 None -177 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
2906372 94008 9 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.4 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3cccnc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL251201 94008 9 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.4 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3cccnc3)c2)CC1 10.1016/j.bmcl.2007.09.016
2284 3133 27 None -12 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -12 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -12 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -12 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -12 28 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
156019279 177399 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 338 3 0 4 3.5 COc1cc2c3c(c1OC)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4645997 177399 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 338 3 0 4 3.5 COc1cc2c3c(c1OC)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
6473679 42442 27 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
CHEMBL1501353 42442 27 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
57391624 71225 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949972 71225 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963102 71225 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmc.2011.12.039
44591029 190397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 511 7 0 6 5.6 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(CCCc4ccccc4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518639 190397 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 511 7 0 6 5.6 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(CCCc4ccccc4)CC3)nc12 10.1016/j.bmcl.2008.12.107
2843443 117429 18 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 380 2 0 2 5.3 Brc1ccc2c(c1)c1c3n2CCN(Cc2ccccc2)C3CCC1 10.1016/j.bmcl.2015.03.049
CHEMBL3403336 117429 18 None -1 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 380 2 0 2 5.3 Brc1ccc2c(c1)c1c3n2CCN(Cc2ccccc2)C3CCC1 10.1016/j.bmcl.2015.03.049
162652495 179880 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCCCC3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4752848 179880 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCCCC3)cccc21 10.1016/j.ejmech.2020.112916
155536152 171573 0 None 9 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 368 4 1 7 2.1 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4473083 171573 0 None 9 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 368 4 1 7 2.1 CN1CCN(c2nc(N)nc(COc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
155546194 172945 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4530840 172945 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
11661320 93678 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 8 1 4 4.7 CN1CCN(c2ccc(OCc3ccccc3)c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL249196 93678 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 8 1 4 4.7 CN1CCN(c2ccc(OCc3ccccc3)c(NCCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
58258789 128472 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4cccnc4)c31)C1CCC(C2)N1 nan
CHEMBL3669671 128472 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4cccnc4)c31)C1CCC(C2)N1 nan
155554036 173629 0 None 18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4548041 173629 0 None 18 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
127045872 139479 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 431 5 0 8 2.9 Cc1noc(C)c1-c1cc(N2CCN(C)CC2)nc2c1ccn2S(=O)(=O)CC(C)C 10.1016/j.bmcl.2016.04.024
CHEMBL3800055 139479 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 431 5 0 8 2.9 Cc1noc(C)c1-c1cc(N2CCN(C)CC2)nc2c1ccn2S(=O)(=O)CC(C)C 10.1016/j.bmcl.2016.04.024
155559811 174266 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4562787 174266 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
1201549 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
333 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
7601 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL1201203 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
CHEMBL438151 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
DB00245 590 22 None -77 20 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 nan
145951815 162266 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 4 1 5 2.2 Fc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172521 162266 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 4 1 5 2.2 Fc1cccc(CCn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
45488151 195235 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm5003952
CHEMBL566213 195235 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm5003952
58258856 127397 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4ccc(N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664743 127397 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4ccc(N)cc4)ccc31)C1CCC(C2)N1 nan
58258805 127419 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(F)c31)C1CCC(C2)N1 nan
CHEMBL3664765 127419 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(F)c31)C1CCC(C2)N1 nan
58258874 128448 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccncc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669647 128448 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ccncc45)ccc31)C1CCC(C2)N1 nan
10947658 28490 0 None -11 16 Human 7.9 pKi = 7.9 Binding
Binding affinities against 5-hydroxytryptamine 6 receptorBinding affinities against 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28490 0 None -11 16 Human 7.9 pKi = 7.9 Binding
Binding affinities against 5-hydroxytryptamine 6 receptorBinding affinities against 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
24768515 126985 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL366151 126985 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1016/j.bmcl.2004.09.003
133 2460 48 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2460 48 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2460 48 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2460 48 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2460 48 None -91 42 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
44438720 93345 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247477 93345 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
155562620 174630 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4571045 174630 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
118626129 165090 0 None -12 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243848 165090 0 None -12 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
118654344 190606 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5189331 190606 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
118654437 191375 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1cccc(Br)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5201088 191375 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1cccc(Br)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
118654343 191778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5207494 191778 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
90469047 185422 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 3 1 6 3.6 O=S(=O)(c1ccccc1Br)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4870340 185422 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 3 1 6 3.6 O=S(=O)(c1ccccc1Br)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
164614987 184144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 540 10 2 7 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850546 184144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 540 10 2 7 5.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
126720403 162060 0 None 37 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169236 162060 0 None 37 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
134130269 141767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 543 9 1 7 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)C4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885238 141767 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 543 9 1 7 3.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)C4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
44403060 70232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194904 70232 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccccc1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403082 71492 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196926 71492 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
164608896 183838 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 183838 0 None 5 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
10042892 5457 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076583 5457 5 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164611615 184070 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 3.8 COC(=O)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4849680 184070 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 3.8 COC(=O)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
164625863 186029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4879036 186029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
145 140 48 None -7 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
1832 140 48 None -7 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
CHEMBL7257 140 48 None -7 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
DB14010 140 48 None -7 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2006.08.068
276 3457 45 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
5312149 3457 45 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
CHEMBL431298 3457 45 None 81 13 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm8009469
45488151 195235 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
CHEMBL566213 195235 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 2 4 3.4 O=C(c1nc2c(N3CCNCC3)cccc2[nH]1)c1cccc2ccccc12 10.1021/jm901672k
155560922 174417 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 444 4 2 5 4.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4566557 174417 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 444 4 2 5 4.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
24783808 175624 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 4 0 6 4.3 CC(C)N1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459372 175624 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 4 0 6 4.3 CC(C)N1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
24783550 176158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460194 176158 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.4 O=S(=O)(c1cc(Cl)ccc1Cl)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
155545832 172904 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2c(C3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4530023 172904 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2c(C3CCNCC3)cccc21 10.1016/j.bmcl.2016.07.055
71502591 117736 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 508 9 1 5 5.6 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409237 117736 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 508 9 1 5 5.6 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
56933434 111605 0 None -21 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289991 111605 0 None -21 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 431 7 1 5 3.8 Cc1cccc(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
66801139 111624 0 None -14 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
CHEMBL3290009 111624 0 None -14 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
66801225 111625 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
CHEMBL3290010 111625 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1csc2ccccc12 10.1021/jm401895u
24768515 126985 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/acs.jmedchem.5b00179
CHEMBL366151 126985 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of radioligand from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ccccc21 10.1021/acs.jmedchem.5b00179
68108531 131145 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692886 131145 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 343 3 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CO)c2oc3c(c2c1)CNCC3 nan
57414522 131173 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COCC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692914 131173 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COCC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25123012 200024 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
CHEMBL606401 200024 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 398 4 2 5 3.4 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)cc1 10.1021/jm901674f
71449798 84000 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165567 84000 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219895 84000 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 438 4 1 5 4.0 CNC1CCc2c(c3cc(OC)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
24967457 83608 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207373 83608 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
44435649 145292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL391713 145292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5082267 213023 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(C(F)(F)F)c1 10.1021/acs.jmedchem.1c00497
44435649 145292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL391713 145292 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 4 0 5 4.8 CCN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25263349 190986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2ccccc2F)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL519513 190986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2ccccc2F)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25117680 198951 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599466 198951 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
16222871 81641 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 5 4.3 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165556 81641 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 5 4.3 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
11003533 116383 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 4 0 5 3.4 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N(C)C 10.1021/jm010943m
CHEMBL338290 116383 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 4 0 5 3.4 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N(C)C 10.1021/jm010943m
10825266 202664 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 5 0 3 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2C(C)C 10.1021/jm990550b
CHEMBL7173 202664 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 5 0 3 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2C(C)C 10.1021/jm990550b
44327453 107425 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 356 3 1 5 2.8 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N 10.1021/jm030030n
CHEMBL319322 107425 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 356 3 1 5 2.8 CO[C@H]1c2cccc3c2c(cn3S(=O)(=O)c2ccc(C)cc2)C[C@@H]1N 10.1021/jm030030n
277 1274 55 None -93 45 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -93 45 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -93 45 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -93 45 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -93 45 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
56944860 158461 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4096479 158461 0 None -56 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 8 2 3 5.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
66801429 159180 0 None -5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 6 2 3 4.5 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4104596 159180 0 None -5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 6 2 3 4.5 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
145983059 165093 0 None -18 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243932 165093 0 None -18 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 492 6 0 6 4.4 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
53327611 69411 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
66800910 111615 0 None -20 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 437 8 1 6 4.0 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3290000 111615 0 None -20 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 437 8 1 6 4.0 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
92042876 150804 0 None -245 10 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 150804 0 None -245 10 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
57403056 70404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950749 70404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3ccc(S(=O)(=O)c4ccccc4)cc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
145963033 160940 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4127861 160940 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
11280771 200113 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606871 200113 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
11464995 60243 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 446 5 0 6 3.3 COc1ccc(OC)c(S(=O)(=O)N2CCC(N3C(=O)OCc4cccc(C)c43)CC2)c1 10.1021/jm049615n
CHEMBL175980 60243 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 446 5 0 6 3.3 COc1ccc(OC)c(S(=O)(=O)N2CCC(N3C(=O)OCc4cccc(C)c43)CC2)c1 10.1021/jm049615n
57400392 69410 0 None -5 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69410 0 None -5 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
127036953 136990 0 None -13 22 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 136990 0 None -13 22 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44438728 93271 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 6 0 3 3.8 COc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247071 93271 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 6 0 3 3.8 COc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
156013326 176920 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4639400 176920 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 350 4 1 4 3.8 COc1cc2c3c(c1OCC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
155513247 169193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 364 7 2 3 4.9 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(F)cc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4438777 169193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 364 7 2 3 4.9 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(F)cc4)o3)c12 10.1016/j.ejmech.2019.111857
10203339 129948 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL368058 129948 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
68108670 131139 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCCNC3 nan
CHEMBL3692880 131139 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCCNC3 nan
155533850 171326 0 None -43 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccc(Cl)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4469633 171326 0 None -43 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 530 7 1 5 5.8 O=c1c(-c2ccc(Cl)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
88597033 131105 0 None - 1 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 4 3.5 [C-]#[N+]c1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692847 131105 0 None - 1 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 4 3.5 [C-]#[N+]c1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
72550645 113590 0 None -186 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 113590 0 None -186 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
142601343 185021 0 None -45 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185021 0 None -45 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
2389 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
5073 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
96 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
CHEMBL85 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
DB00734 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2020.112709
2389 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
5073 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
96 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
CHEMBL85 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
DB00734 3279 114 None -2454 67 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2021.127909
137644687 157843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 523 6 0 5 5.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4089941 157843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 523 6 0 5 5.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCN(Cc3ccccc3)CC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
56944763 111619 0 None -331 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290004 111619 0 None -331 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
68109133 131129 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692870 131129 0 None - 1 Human 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
71574212 85857 0 None -147 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312935 85857 0 None -147 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
16026344 22050 4 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 373 2 0 3 5.0 O=S1(=O)c2ccccc2N(Cc2ccc(Cl)cc2F)c2ccccc21 10.1016/j.bmcl.2015.03.049
CHEMBL1323386 22050 4 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 373 2 0 3 5.0 O=S1(=O)c2ccccc2N(Cc2ccc(Cl)cc2F)c2ccccc21 10.1016/j.bmcl.2015.03.049
71462178 81014 0 None -54 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 437 7 1 4 4.8 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
CHEMBL2159469 81014 0 None -54 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 437 7 1 4 4.8 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc2ccccc2n1 10.1016/j.ejmech.2012.07.043
134157769 153525 0 None -93 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 2 6 4.7 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCO)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3984541 153525 0 None -93 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 2 6 4.7 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCO)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168276579 189774 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 4 1 5 4.2 COc1cccc(Cn2ccc3c(N4CCC(O)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5177167 189774 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 4 1 5 4.2 COc1cccc(Cn2ccc3c(N4CCC(O)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
49836504 18552 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277749 18552 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 360 3 2 5 1.9 O=S(=O)(c1cccc(F)c1)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
49836506 18560 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
CHEMBL1277834 18560 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
2162 41273 97 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
CHEMBL1491 41273 97 None -2 6 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl nan
138691316 174116 0 None -67 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 289 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4559312 174116 0 None -67 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 289 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
44438709 152278 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 7 0 4 2.7 CCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL397380 152278 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 7 0 4 2.7 CCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
49781250 17002 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 673 9 1 9 5.1 COc1ccc(N(S(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256256 17002 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 673 9 1 9 5.1 COc1ccc(N(S(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
164625711 185750 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4874914 185750 0 None -64 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2021.128028
12051078 111676 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL329046 111676 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
52912977 127379 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127379 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
12051078 111676 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
CHEMBL329046 111676 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 348 5 0 3 4.7 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN(C)C 10.1021/jm030030n
21514234 167976 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2006.12.089
CHEMBL435534 167976 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2006.12.089
168268997 189378 0 None -19 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 410 7 3 8 2.4 Nc1nc(N)nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5170808 189378 0 None -19 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 410 7 3 8 2.4 Nc1nc(N)nc(NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
57396850 71180 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71180 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71180 0 None -8 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
71727068 90836 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401934 90836 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401938 90836 0 None -31 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cc(CN4CCN(c5ccccc5OC)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
168274079 189695 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 403 3 0 4 5.1 Clc1cccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5175763 189695 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 403 3 0 4 5.1 Clc1cccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
11716331 154374 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 4 1 5 2.5 CN1CCN(c2ccc(C#N)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL400922 154374 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 4 1 5 2.5 CN1CCN(c2ccc(C#N)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
168295839 191647 0 None -165 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 370 9 3 8 1.8 Nc1nc(N)nc(NCCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5205324 191647 0 None -165 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 370 9 3 8 1.8 Nc1nc(N)nc(NCCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
145985050 165137 0 None -1380 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245263 165137 0 None -1380 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
162663591 181400 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 14 0 5 7.2 C#CCN(C)Cc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4780366 181400 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 14 0 5 7.2 C#CCN(C)Cc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
145961507 160924 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4127652 160924 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
11016205 203060 1 None -107 5 Human 6.9 pKi = 6.9 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
CHEMBL74756 203060 1 None -107 5 Human 6.9 pKi = 6.9 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
56595535 65318 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
CHEMBL1834239 65318 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 408 4 1 3 3.6 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(F)cc1 10.1021/jm200466r
155569396 175564 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 279 2 1 2 4.1 CCn1cncc1-c1c[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4592256 175564 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 279 2 1 2 4.1 CCn1cncc1-c1c[nH]c2ccc(C(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
58258830 127402 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664748 127402 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc(F)c4)ccc31)C1CCC(C2)N1 nan
44568101 190843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 446 5 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL519299 190843 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 446 5 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
145952652 161864 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)c(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166040 161864 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)c(F)c1 10.1016/j.ejmech.2017.12.053
57325520 71194 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949963 71194 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1962945 71194 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
57395190 69406 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 413 2 1 4 4.3 CC1(C(F)(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935596 69406 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 413 2 1 4 4.3 CC1(C(F)(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
44386718 167974 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3ccccc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL435524 167974 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3ccccc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
86294717 113686 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 300 3 2 2 4.2 CC(Nc1ccc2c(c1)CCNCC2)c1ccccc1Cl 10.1021/jm5003952
CHEMBL3329455 113686 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 300 3 2 2 4.2 CC(Nc1ccc2c(c1)CCNCC2)c1ccccc1Cl 10.1021/jm5003952
52913345 127390 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 395 3 1 5 3.4 CN(C)c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664736 127390 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 395 3 1 5 3.4 CN(C)c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258877 127423 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 410 4 1 5 4.1 CC(C)Oc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664769 127423 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 410 4 1 5 4.1 CC(C)Oc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258851 127424 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccc4)c31)C1CCC(C2)N1 nan
CHEMBL3664770 127424 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 458 5 1 5 4.9 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccc4)c31)C1CCC(C2)N1 nan
58258795 128493 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669692 128493 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
44389075 63782 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 390 3 1 4 4.0 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL180823 63782 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 390 3 1 4 4.0 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
53326022 59825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642863 59825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739645 59825 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 7 1 5 3.5 CN(C)CCN(C)Cc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
155560188 174361 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ncccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4565216 174361 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ncccc2c1 10.1021/acsmedchemlett.6b00056
155537074 171704 0 None 9 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c12 10.1016/j.ejmech.2019.111857
CHEMBL4474618 171704 0 None 9 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1cccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c12 10.1016/j.ejmech.2019.111857
90469188 183896 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 434 4 1 6 4.0 CC(C)c1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)cc1 10.1021/acs.jmedchem.1c00224
CHEMBL4847012 183896 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 434 4 1 6 4.0 CC(C)c1ccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)cc1 10.1021/acs.jmedchem.1c00224
90469252 184444 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 442 3 1 6 4.0 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4855043 184444 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 442 3 1 6 4.0 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
44403070 72077 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL198766 72077 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10141477 139728 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380556 139728 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 494 5 0 4 5.6 O=S(=O)(c1ccccc1Br)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57393468 69409 0 None -6 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69409 0 None -6 2 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
44420490 141112 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 0 4 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.08.068
CHEMBL385330 141112 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 0 4 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.08.068
155514459 169302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.9 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4440402 169302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.9 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155542461 172571 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 442 5 2 6 3.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4521199 172571 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 442 5 2 6 3.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155566855 175668 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4586353 175668 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594758 175668 0 None 7 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
24763430 62290 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
CHEMBL1783582 62290 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 397 4 1 4 4.3 CC(C)c1ccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)cc1 10.1016/j.bmcl.2009.04.108
23655463 88262 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL235987 88262 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1021/jm070521y
68116185 131177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.7 COCc1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692918 131177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 4 1 5 3.7 COCc1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
58158738 138433 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785231 138433 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 3 3 5 0.6 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCNCC2 10.1016/j.bmcl.2016.02.001
137630083 160497 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4101418 160497 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4116501 160497 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
162644013 181257 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4778418 181257 0 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
58158719 138462 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785431 138462 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1ccc(O)c(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595403 65307 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834227 65307 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 356 5 1 3 2.7 CCCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
25024144 62627 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785060 62627 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
49799667 10812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172795 10812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 456 5 1 9 3.8 O=S(=O)(c1cccc(Cl)c1)c1nnn2c1nc(NCc1cccnc1)c1sccc12 10.1016/j.bmc.2010.05.051
275 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
3246 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
5312144 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
CHEMBL46071 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
25025118 62636 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 1 5 3.4 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCNCC4)ccc32)cc1 10.1021/ml100101u
CHEMBL1785069 62636 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 5 1 5 3.4 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCNCC4)ccc32)cc1 10.1021/ml100101u
11338378 60473 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3ccc4ccccc4c3)cccc21 10.1021/jm049615n
CHEMBL176117 60473 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3ccc4ccccc4c3)cccc21 10.1021/jm049615n
162675700 182879 0 None -16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4799043 182879 0 None -16 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 650 10 3 7 4.7 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2cc(Br)c(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
162661064 181276 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 568 13 0 5 6.8 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4778708 181276 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 568 13 0 5 6.8 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
90656157 110339 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 292 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260789 110339 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 292 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
90656172 110354 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260805 110354 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
118731505 117610 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 557 9 1 6 5.8 O=C1CCc2ccc(OCCCCN3CCC(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3407518 117610 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 557 9 1 6 5.8 O=C1CCc2ccc(OCCCCN3CCC(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
68281136 111563 0 None -15 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 422 7 1 7 2.8 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289950 111563 0 None -15 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 422 7 1 7 2.8 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
66801455 111577 0 None -34 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 8 2.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289964 111577 0 None -34 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 470 8 1 8 2.8 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
56944667 111606 0 None -93 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289992 111606 0 None -93 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 445 8 1 5 4.2 Cc1cccc(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
11270131 60474 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL176134 60474 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.9 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL5074880 212568 0 None -147 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2337 3205 72 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3205 72 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3205 72 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3205 72 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3205 72 None -54 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
2927683 161653 9 None 2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 8 1 2 6.0 CC(NCCC(Cc1ccccc1)c1ccco1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4162688 161653 9 None 2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 8 1 2 6.0 CC(NCCC(Cc1ccccc1)c1ccco1)c1ccc(Cl)cc1 10.1016/j.ejmech.2018.04.010
145986752 166723 0 None -3 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 166723 0 None -3 17 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
136118729 92630 0 None -12 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 92630 0 None -12 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
136118616 75895 0 None -14 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 75895 0 None -14 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
10088284 65979 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 334 4 1 4 3.1 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL184884 65979 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 334 4 1 4 3.1 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
164622805 185281 0 None -25 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185281 0 None -25 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
155533648 171319 0 None -10 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 486 9 0 6 4.7 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4469539 171319 0 None -10 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 486 9 0 6 4.7 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
126720412 162371 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 4 1 5 3.8 Cc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4174125 162371 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 4 1 5 3.8 Cc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
13069623 120097 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360994 120097 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546108 120097 0 None -616 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 396 6 0 8 1.0 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
3042 1386 31 None -51 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
355 1386 31 None -51 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
868 1386 31 None -51 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
CHEMBL1123 1386 31 None -51 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
DB00804 1386 31 None -51 15 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC nan
165193 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3138 60 None -158 42 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
44403101 71653 0 None -223 6 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL197408 71653 0 None -223 6 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
9949258 137074 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1c2n(c3ccccc13)S(=O)(=O)c1ccccc1-2 10.1016/j.bmcl.2006.08.068
CHEMBL375594 137074 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1c2n(c3ccccc13)S(=O)(=O)c1ccccc1-2 10.1016/j.bmcl.2006.08.068
68108522 131164 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 2 3 3.8 OC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692905 131164 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 2 3 3.8 OC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
4098 32289 24 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1255739 32289 24 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
CHEMBL1411979 32289 24 None -22 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 nan
164611085 184045 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 373 8 2 4 3.5 O=c1[nH]c2c(OCCNCc3ccccc3)cccc2n1Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4849430 184045 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 373 8 2 4 3.5 O=c1[nH]c2c(OCCNCc3ccccc3)cccc2n1Cc1ccccc1 10.1016/j.ejmech.2021.113792
71727064 101935 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
CHEMBL3039719 101935 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
CHEMBL3216145 101935 0 None -3 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 372 4 1 5 2.7 O=c1c2ccc(Cl)cc2oc2c(CN3CCN(CCO)CC3)cccc12 10.1016/j.bmcl.2013.05.062
57400830 68095 0 None -77 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917358 68095 0 None -77 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
155527359 170672 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 5 2 2 5.1 c1ccc(-c2ccc(NCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4459786 170672 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 5 2 2 5.1 c1ccc(-c2ccc(NCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
57396848 71192 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71192 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71192 0 None -4 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
160510 100658 36 None -5 4 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL1506260 100658 36 None -5 4 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL295234 100658 36 None -5 4 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
118736371 118438 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 6 0 9 2.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423335 118438 0 None -38 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 6 0 9 2.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
164613297 184034 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4849230 184034 0 None -1 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
137652310 156708 0 None -50 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076525 156708 0 None -50 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
11110394 179129 15 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1cc(-c2ccccc2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4743932 179129 15 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1cc(-c2ccccc2)c2ccccc21 10.1016/j.ejmech.2020.112916
164618556 185411 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 479 8 1 5 4.4 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4870158 185411 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 479 8 1 5 4.4 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
56593936 65366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834352 65366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
56593936 65366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834352 65366 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(C)(C)C=N1 10.1021/jm200466r
155515890 169435 0 None -46 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 414 8 0 4 4.6 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4442385 169435 0 None -46 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 414 8 0 4 4.6 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
155553005 173507 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 2 4 4.7 CC(=O)Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4544414 173507 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 7 2 4 4.7 CC(=O)Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
90654836 112197 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233667 112197 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304308 112197 0 None -630 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 464 9 0 5 3.8 COc1ccccc1N1CCN(CCCCCN2C(=O)N(C)C(=O)C2(C)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
164614127 184554 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 4.7 Cc1cccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4856695 184554 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 4.7 Cc1cccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
71451455 81006 0 None -8 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 9 1 5 4.1 CSc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159461 81006 0 None -8 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 9 1 5 4.1 CSc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
162668604 182004 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
CHEMBL4788022 182004 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 587 11 2 7 4.4 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Br 10.1016/j.ejmech.2016.05.048
57394663 71211 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949973 71211 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963031 71211 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 457 8 1 4 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2011.12.039
11674694 94372 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL253502 94372 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
58258784 127441 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ncccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664788 127441 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5ncccc45)ccc31)C1CCC(C2)N1 nan
90178632 144895 0 None -9 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 468 10 1 5 4.1 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3914155 144895 0 None -9 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 468 10 1 5 4.1 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155538814 172692 0 None 4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4524981 172692 0 None 4 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 334 4 1 7 1.4 CN1CCN(c2nc(N)nc(COc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2019.06.022
5280953 96913 102 None -1 8 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
CHEMBL269538 96913 102 None -1 8 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 212 1 1 2 3.0 COc1ccc2c(c1)[nH]c1c(C)nccc12 10.1016/j.bmcl.2003.09.027
118626120 165236 0 None -245 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4247770 165236 0 None -245 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
3158 55974 21 None -851 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -851 20 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
164615296 184838 0 None -19 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 465 9 0 5 5.6 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCCCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4861311 184838 0 None -19 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 465 9 0 5 5.6 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCCCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
2866185 93905 9 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 286 7 3 5 2.6 NCCNc1ccc([N+](=O)[O-])c(NCc2ccccc2)c1 10.1016/j.bmcl.2007.09.016
CHEMBL250663 93905 9 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 286 7 3 5 2.6 NCCNc1ccc([N+](=O)[O-])c(NCc2ccccc2)c1 10.1016/j.bmcl.2007.09.016
74763017 113220 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
CHEMBL3323289 113220 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
52913098 127384 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc(CN)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664730 127384 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc(CN)cc4)ccc31)C1CCC(C2)N1 nan
58258820 127439 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccncc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664786 127439 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ccncc54)ccc31)C1CCC(C2)N1 nan
58258833 127446 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127446 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
10472143 118772 0 None -33 16 Human 7.8 pKi = 7.8 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 118772 0 None -33 16 Human 7.8 pKi = 7.8 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
11849787 138709 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378892 138709 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
1613 2316 44 None -4 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
205 2316 44 None -4 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
3964 2316 44 None -4 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
CHEMBL831 2316 44 None -4 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
DB00408 2316 44 None -4 44 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm030030n
118654431 191022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5195558 191022 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1cccc(Cl)c1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
164609469 183812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 550 13 2 8 4.1 CCN(C)C(=O)Oc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
CHEMBL4845823 183812 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 550 13 2 8 4.1 CCN(C)C(=O)Oc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
134130529 141603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 8 0 6 4.1 CN(CCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3883443 141603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 8 0 6 4.1 CN(CCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
10140915 139825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL380772 139825 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 484 5 0 4 6.2 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
46880705 5480 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(Cl)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076687 5480 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(Cl)cc12 10.1016/j.bmcl.2010.01.073
52912973 70405 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70405 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164612119 184049 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 1 5 4.4 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4849477 184049 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 1 5 4.4 Cc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
44420569 84472 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(CCN(C)C)cn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
CHEMBL223637 84472 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(CCN(C)C)cn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2006.08.068
11849787 138709 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
CHEMBL378892 138709 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 4 1.8 CN(C)CCc1ccn(S(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
155533573 171301 0 None 346 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4469147 171301 0 None 346 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
155537227 171720 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 458 5 2 5 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4474829 171720 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 458 5 2 5 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc4ccccc34)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
127047536 139354 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 506 4 0 6 5.0 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCCCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3799330 139354 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 506 4 0 6 5.0 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCCCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
45484307 195154 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565753 195154 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 5 0 6 2.5 CN(C)CCn1cc(S(=O)(=O)c2cccs2)c2cccnc21 10.1016/j.bmc.2009.05.055
24771124 183752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484333 183752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 1 6 4.2 O=C(CCN1CCCCC1)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
90656167 110349 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 3 3.2 O=C1OC(c2ccccc2F)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260800 110349 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 3 3.2 O=C1OC(c2ccccc2F)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
57396850 71180 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949762 71180 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962863 71180 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 3 1 4 4.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2011.12.026
66801613 111558 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289945 111558 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
16222868 81617 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Br)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165533 81617 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Br)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
25263351 183790 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1cccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484534 183790 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1cccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
10228179 63027 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 489 6 2 5 5.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCOCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL179492 63027 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 489 6 2 5 5.0 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCOCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
162650168 179526 0 None -25 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4748379 179526 0 None -25 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
23653133 56390 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 3 0 5 3.4 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642415 56390 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 3 0 5 3.4 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
25263306 183655 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 307 4 1 4 2.9 Cc1c(OCc2cccc(C#N)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483558 183655 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 307 4 1 4 2.9 Cc1c(OCc2cccc(C#N)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL5089348 213429 0 None -7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.1c00497
44395500 122061 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.7 CNCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL360181 122061 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.7 CNCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
10024749 158020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 5 0 6 2.9 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4091721 158020 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 5 0 6 2.9 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/acs.jmedchem.6b01662
16222447 81614 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165530 81614 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
16222763 81644 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 4 4.6 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165559 81644 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 4 0 4 4.6 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
16222761 81610 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165526 81610 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 372 3 0 4 3.4 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
275 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
3246 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
5312144 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
CHEMBL46071 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
275 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
3246 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
5312144 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
CHEMBL46071 3308 6 None -1 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
164610188 184472 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 184472 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
75306277 108767 0 None -7 23 Human 7.8 pKi = 7.8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108767 0 None -7 23 Human 7.8 pKi = 7.8 Binding
Binding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT6 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
46890294 7082 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 413 5 2 4 3.2 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ncc[nH]1 10.1016/j.bmcl.2010.03.110
CHEMBL1085409 7082 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 413 5 2 4 3.2 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ncc[nH]1 10.1016/j.bmcl.2010.03.110
44425706 150075 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL395525 150075 0 None -10 5 Human 7.8 pKi = 7.8 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
16019553 10606 7 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170871 10606 7 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 479 6 1 8 4.4 CC(C)CCNc1nc2c(S(=O)(=O)c3ccc(Br)cc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53322547 56391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642416 56391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL4115766 211180 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL None None None None nan
56944862 156227 0 None -33 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4070715 156227 0 None -33 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
137633644 156013 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 453 5 0 6 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068315 156013 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 453 5 0 6 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(OC(F)(F)F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
54586997 62209 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782363 62209 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
12005903 50950 12 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
CHEMBL1580288 50950 12 None 2 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 482 5 0 7 4.0 CCS(=O)(=O)c1nc(S(=O)(=O)c2ccc(Cl)cc2)c(N2CCc3ccccc3C2)s1 10.1016/j.bmcl.2015.03.049
90656174 110356 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260807 110356 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CNCC2 10.1016/j.bmcl.2014.03.049
118731504 117733 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 1 4 6.6 O=C1CCc2ccc(OCCCCN3CCC(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409234 117733 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 1 4 6.6 O=C1CCc2ccc(OCCCCN3CCC(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118731506 117734 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 11 2 4 5.6 O=C1CCc2ccc(OCCCCNCCc3cn(Cc4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409235 117734 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 11 2 4 5.6 O=C1CCc2ccc(OCCCCNCCc3cn(Cc4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
156010396 176553 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 392 5 1 4 4.2 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4633765 176553 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 392 5 1 4 4.2 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
90644074 111580 0 None -151 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289967 111580 0 None -151 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 414 7 1 6 2.6 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
134151118 151669 0 None -72 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 498 12 1 4 5.4 CN(C)Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3968569 151669 0 None -72 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 498 12 1 4 5.4 CN(C)Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
162643605 181119 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccncc3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4776760 181119 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccncc3)cccc21 10.1016/j.ejmech.2020.112916
52912977 127379 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127379 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL5083505 213094 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00497
11384694 127537 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 3 0 5 3.5 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3cccnc23)CC1 10.1021/jm049615n
CHEMBL366515 127537 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 3 0 5 3.5 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3cccnc23)CC1 10.1021/jm049615n
2771422 93645 15 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 5 2 6 2.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1cccnc1 10.1016/j.bmcl.2007.09.016
CHEMBL249032 93645 15 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 5 2 6 2.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1cccnc1 10.1016/j.bmcl.2007.09.016
2247 502 77 None -53 41 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -53 41 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -53 41 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -53 41 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -53 41 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
72550642 113579 0 None -173 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 113579 0 None -173 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6 (unknown origin)Binding affinity to 5-HT6 (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
57402588 68084 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917347 68084 0 None -6 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
155528725 170824 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 2 2 5.2 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)s2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4462131 170824 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 2 2 5.2 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)s2)cc1 10.1016/j.ejmech.2019.111857
168277941 190089 0 None -72 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 374 9 2 4 1.8 NS(=O)(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5181868 190089 0 None -72 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 374 9 2 4 1.8 NS(=O)(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
57403841 71210 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949968 71210 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963030 71210 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
12017578 108084 17 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2[nH]cc(CCN(C)C)c12 10.1021/jm030030n
CHEMBL32029 108084 17 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2[nH]cc(CCN(C)C)c12 10.1021/jm030030n
68108408 131136 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692877 131136 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
50878551 90314 60 None -2 18 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90314 60 None -2 18 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL5085390 213191 0 None -12 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc3cc(Cl)ccc3c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
21509921 103979 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
145946714 166997 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4213352 166997 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300399 166997 0 None -109 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
57395084 71207 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949964 71207 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963027 71207 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.bmc.2011.12.039
21509921 103979 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 103979 0 None -15 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
164610373 184646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 480 8 2 6 4.0 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4858014 184646 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 480 8 2 6 4.0 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
57396088 70423 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950768 70423 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 nan
71449644 81029 0 None -15 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 436 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159484 81029 0 None -15 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 436 7 1 4 3.3 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
57400477 69398 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935588 69398 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
57396088 70423 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950768 70423 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4cccnc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11573559 94401 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 1 2 3 3.7 CC1(c2ccc(N)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253709 94401 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 1 2 3 3.7 CC1(c2ccc(N)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
57398615 71205 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71205 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71205 0 None -6 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
1296368 50549 16 None 1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 458 5 2 5 6.0 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccccc1 10.1016/j.bmcl.2015.03.049
CHEMBL1576791 50549 16 None 1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 458 5 2 5 6.0 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccccc1 10.1016/j.bmcl.2015.03.049
155530285 170925 0 None 20 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 6 1 7 3.9 COc1ccc2c(c1)c(-c1c(C)nc(N)n1CC(F)F)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4463737 170925 0 None 20 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 6 1 7 3.9 COc1ccc2c(c1)c(-c1c(C)nc(N)n1CC(F)F)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
25107716 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
8436 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL522691 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assayDisplacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1016/j.ejmech.2016.05.005
25107716 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 2319 35 None -2754 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
7125890 117435 11 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 408 4 1 4 5.8 Cc1ccc(Nc2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403341 117435 11 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 408 4 1 4 5.8 Cc1ccc(Nc2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)cc1 10.1016/j.bmcl.2015.03.049
162670887 182387 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
CHEMBL4793078 182387 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 543 11 2 7 4.2 COc1ccc(S(=O)(=O)NCCN2CCC(CCC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1Cl 10.1016/j.ejmech.2016.05.048
137632931 156035 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
CHEMBL4068577 156035 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
156016142 177174 0 None -8 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4642594 177174 0 None -8 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 506 8 0 6 5.3 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
162671683 182308 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 559 12 2 6 4.9 C[C@H](NCc1ccc(OCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4792096 182308 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 559 12 2 6 4.9 C[C@H](NCc1ccc(OCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
44369599 119193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 461 5 2 5 2.9 COc1ccc(S(=O)(=O)Nc2c(F)cc(Br)cc2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL347335 119193 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 461 5 2 5 2.9 COc1ccc(S(=O)(=O)Nc2c(F)cc(Br)cc2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
134148634 147991 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
CHEMBL3938498 147991 0 None 19 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2cc3c(cc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
134150535 151091 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3963688 151091 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
134151926 152902 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3979230 152902 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
46889915 7336 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)Cc3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086546 7336 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 315 4 1 3 3.0 NC[C@@H]1CCCc2cc(S(=O)(=O)Cc3ccccc3)ccc21 10.1016/j.bmcl.2010.03.110
24865727 192511 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT6 receptorDisplacement of radioligand from human cloned 5HT6 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 192511 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT6 receptorDisplacement of radioligand from human cloned 5HT6 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
156013801 176708 0 None -93 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 278 1 0 2 3.5 CN(C)c1ccc2c(c1)-c1cccc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4636329 176708 0 None -93 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 278 1 0 2 3.5 CN(C)c1ccc2c(c1)-c1cccc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
72198011 89415 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL2377591 89415 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
315017 203972 102 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 257 2 0 3 2.9 O=S(=O)(c1ccccc1)n1ccc2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL82224 203972 102 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 257 2 0 3 2.9 O=S(=O)(c1ccccc1)n1ccc2ccccc21 10.1016/j.ejmech.2020.112916
72198011 89415 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
CHEMBL2377591 89415 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
118736370 118437 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 7 0 9 2.3 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423334 118437 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 483 7 0 9 2.3 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
2470 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
2470 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 3596 46 None -7413 59 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
45488143 196089 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm5003952
CHEMBL571762 196089 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm5003952
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2005.01.031
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmcl.2004.05.076
145 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
1832 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
CHEMBL7257 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
DB14010 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00453-4
12147017 165505 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL425714 165505 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 412 6 0 5 3.9 CN(C)CCn1cc(S(=O)(=O)c2ccccc2OC(F)(F)F)c2ccccc21 10.1016/j.bmcl.2004.09.003
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1007/s00044-004-0121-8
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1016/j.bmc.2009.08.006
145 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
1832 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
CHEMBL7257 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
DB14010 140 48 None -7 29 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm030030n
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm030030n
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
134131115 141675 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 9 1 6 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884154 141675 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 488 9 1 6 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130035 154056 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884254 154056 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3991406 154056 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 585 11 1 7 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
44403076 71459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL196792 71459 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
57402187 69407 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69407 0 None 11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
164610188 184472 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 184472 0 None 6 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
46880531 6222 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081793 6222 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 416 5 0 5 4.3 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(OC)ccc32)C1 10.1016/j.bmcl.2010.01.073
52942395 17739 0 None -30 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL1259203 17739 0 None -30 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
164619953 184897 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4862131 184897 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(Cl)cc3)cccc21 10.1016/j.ejmech.2021.113792
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm070910s
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm8009469
45488143 196089 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
CHEMBL571762 196089 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2c(Cc3nc4c(N5CCNCC5)cccc4[nH]3)cccc2c1 10.1021/jm901672k
155531455 171087 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 452 7 2 6 4.2 CCC(=O)Nc1nc(CC)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4466071 171087 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 452 7 2 6 4.2 CCC(=O)Nc1nc(CC)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
23655288 146703 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccccc2I)c2ccccc12 10.1021/jm070521y
CHEMBL392844 146703 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 426 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2ccccc2I)c2ccccc12 10.1021/jm070521y
127047776 139405 0 None 34 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 412 5 0 6 3.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799638 139405 0 None 34 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 412 5 0 6 3.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
90656166 110348 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 308 2 1 3 3.1 O=C1OC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260799 110348 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 308 2 1 3 3.1 O=C1OC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
71151925 117760 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 489 9 0 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409261 117760 0 None 3 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 489 9 0 6 4.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
12 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
6918513 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/acs.jmedchem.5b00179
11372111 200079 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
CHEMBL606706 200079 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 2 3 3.6 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3)cc12 10.1021/jm049243i
57414392 131100 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692842 131100 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
68108812 131130 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 392 2 1 5 4.3 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)C2CCC(C4)N2)c2ccccc12 nan
CHEMBL3692871 131130 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 392 2 1 5 4.3 Cc1cn(S(=O)(=O)c2ccc3oc4c(c3c2)C2CCC(C4)N2)c2ccccc12 nan
68108636 131152 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131152 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115683 131208 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692949 131208 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
16222655 81609 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165525 81609 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL5090557 213496 0 None -23 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccccc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
137656063 158145 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4093110 158145 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
56595402 65306 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL5082182 213021 1 None -3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1cccc(Cl)c1 10.1021/acs.jmedchem.1c00497
44544596 176851 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 354 3 2 5 2.9 O=S(=O)(Nc1ccc2[nH]ccc2c1)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
CHEMBL4638578 176851 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 354 3 2 5 2.9 O=S(=O)(Nc1ccc2[nH]ccc2c1)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
53327611 69411 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None -1 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
164619216 185082 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185082 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
44286416 140886 0 None -15 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL38409 140886 0 None -15 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 448 8 0 6 4.3 O=C1c2ccccc2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
54582159 62210 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782364 62210 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 300 2 1 3 3.3 Fc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
58158717 138517 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 415 3 2 3 3.2 CCN/C(=N\S(=O)(=O)c1ccc2[nH]c(C(F)(F)F)cc2c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786071 138517 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 415 3 2 3 3.2 CCN/C(=N\S(=O)(=O)c1ccc2[nH]c(C(F)(F)F)cc2c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
66801354 111591 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289977 111591 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 450 7 1 6 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
117209857 184555 1 None -3 8 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 184555 1 None -3 8 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
58622472 180611 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccccc3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4761081 180611 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2c(-c3ccccc3)cccc21 10.1016/j.ejmech.2020.112916
162644220 181191 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 573 13 2 6 5.3 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4777701 181191 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 573 13 2 6 5.3 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
126720427 161994 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 405 4 1 5 3.8 Fc1ccc(-c2nc3c(N4CCNCC4)ccnc3n2Cc2cccc(F)c2)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4168070 161994 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 405 4 1 5 3.8 Fc1ccc(-c2nc3c(N4CCNCC4)ccnc3n2Cc2cccc(F)c2)cc1 10.1016/j.ejmech.2017.12.053
134139826 145999 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3922670 145999 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155538367 171815 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 263 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4476372 171815 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 263 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
134133483 142677 0 None -87 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 614 16 1 7 5.5 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3896355 142677 0 None -87 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 614 16 1 7 5.5 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
3142696 153388 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 2 6 2.8 Cc1ccccc1OCCNc1cc(N2CCNCC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL398336 153388 12 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 356 7 2 6 2.8 Cc1ccccc1OCCNc1cc(N2CCNCC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
10296699 62068 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 9 2 3 5.4 CCN(CC)CCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL177970 62068 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 9 2 3 5.4 CCN(CC)CCCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
10113852 62843 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL178985 62843 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 435 6 2 4 4.0 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCOCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
134135516 143641 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3904094 143641 0 None -21 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3ncccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11559141 154328 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 338 4 1 4 2.6 CC(=O)N(Cc1ccccc1)c1ccc(N2CCN(C)CC2)cc1N 10.1016/j.bmcl.2007.09.016
CHEMBL400660 154328 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 338 4 1 4 2.6 CC(=O)N(Cc1ccccc1)c1ccc(N2CCN(C)CC2)cc1N 10.1016/j.bmcl.2007.09.016
156018383 177349 0 None -134 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2020.115459
CHEMBL4645308 177349 0 None -134 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2020.115459
44413644 79831 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1cccc2c1c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2006.04.094
CHEMBL213800 79831 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1cccc2c1c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2006.04.094
24967097 83614 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 453 4 0 5 4.4 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207379 83614 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 453 4 0 5 4.4 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
126720406 161876 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 393 5 1 6 3.5 COc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166211 161876 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 393 5 1 6 3.5 COc1cccc(Cn2c(CC(C)(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
126720370 162484 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 409 4 1 6 4.3 Clc1cccc(Cn2c(-c3cccs3)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175926 162484 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 409 4 1 6 4.3 Clc1cccc(Cn2c(-c3cccs3)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
49782361 16995 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 8 6.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(S(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256249 16995 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 8 6.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(S(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
11270546 130368 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 3 0 5 3.9 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4cccnc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL368557 130368 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 3 0 5 3.9 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4cccnc34)CC1)C(=O)OC2 10.1021/jm049615n
155533534 171318 0 None -128 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4469537 171318 0 None -128 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 514 7 1 5 5.3 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccccc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
22549784 117434 5 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 418 4 0 4 4.9 COc1cccc(-n2cc(C(=O)N(C)c3cccc(Cl)c3)c3ccccc3c2=O)c1 10.1016/j.bmcl.2015.03.049
CHEMBL3403340 117434 5 None -1 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 418 4 0 4 4.9 COc1cccc(-n2cc(C(=O)N(C)c3cccc(Cl)c3)c3ccccc3c2=O)c1 10.1016/j.bmcl.2015.03.049
3303 2213 41 None -2398 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 2213 41 None -2398 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 2213 41 None -2398 15 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
57393365 71206 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
138691314 164084 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4216263 164084 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
162666007 181700 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 341 3 0 4 3.3 O=S(=O)(N1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4783954 181700 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 341 3 0 4 3.3 O=S(=O)(N1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
57325521 71226 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949977 71226 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1963103 71226 0 None -354 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
68115818 131222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 442 2 0 5 4.3 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4cn(C)c5ccccc45)cc3c2C1 nan
CHEMBL3692963 131222 0 None - 1 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 442 2 0 5 4.3 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4cn(C)c5ccccc45)cc3c2C1 nan
154956306 179084 0 None -18 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
CHEMBL4743324 179084 0 None -18 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 435 6 0 6 4.5 Cn1ccc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2c1=O 10.1016/j.ejmech.2020.112709
145980271 165939 0 None -3 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 165939 0 None -3 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
53325242 56775 0 None -8 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56775 0 None -8 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
138691314 164084 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1039/C8MD00313K
CHEMBL4216263 164084 1 None -275 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 337 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(I)cc12 10.1039/C8MD00313K
10658892 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1016/j.bmcl.2004.01.071
CHEMBL7228 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1016/j.bmcl.2004.01.071
10658892 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm990550b
CHEMBL7228 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm990550b
10658892 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm030030n
CHEMBL7228 202753 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 258 3 1 2 3.2 COc1ccc2[nH]c3c(c2c1)C(CN(C)C)CCC3 10.1021/jm030030n
53328001 111209 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286592 111209 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
145988693 166613 0 None -66 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 166613 0 None -66 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
42 2032 50 None -2951 17 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
56971 2032 50 None -2951 17 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
CHEMBL8412 2032 50 None -2951 17 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2021.128028
155544811 175977 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4567345 175977 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4597228 175977 0 None -29 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
145985233 164971 0 None -100 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241050 164971 0 None -100 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
5311507 193147 37 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm2011657
CHEMBL53904 193147 37 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm2011657
53328001 111209 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286592 111209 0 None 17 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
145965840 163464 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 425 5 1 4 3.8 O=C1Nc2ccccc2C12CCN(CCN1CCC(Oc3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4208468 163464 0 None -14 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 425 5 1 4 3.8 O=C1Nc2ccccc2C12CCN(CCN1CCC(Oc3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168293886 191582 0 None -24 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 488 8 0 4 4.5 O=S1(=O)N(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2N1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5204088 191582 0 None -24 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 488 8 0 4 4.5 O=S1(=O)N(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2N1CCC3 10.1016/j.ejmech.2022.114319
53324045 56776 0 None -44 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 56776 0 None -44 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
155522233 170093 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 363 7 2 5 4.7 COc1ccc2occ(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4451494 170093 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 363 7 2 5 4.7 COc1ccc2occ(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
155552054 173439 0 None -36 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)c1 10.1016/j.bmcl.2019.06.029
CHEMBL4542754 173439 0 None -36 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)c1 10.1016/j.bmcl.2019.06.029
52913222 127388 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664734 127388 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258796 127418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 3.9 CCc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664764 127418 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 3.9 CCc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258806 127443 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127443 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
9800707 202798 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm010943m
CHEMBL72574 202798 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm010943m
11849204 138561 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 306 6 2 4 2.0 COc1ccc(NS(=O)(=O)c2ccccc2)cc1CCN 10.1021/jm060469q
CHEMBL378656 138561 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 306 6 2 4 2.0 COc1ccc(NS(=O)(=O)c2ccccc2)cc1CCN 10.1021/jm060469q
10171 57 15 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
272 57 15 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
CHEMBL274384 57 15 None -8 6 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
16116896 59824 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642861 59824 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739644 59824 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NCC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
53320746 59834 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642854 59834 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739685 59834 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
53319443 59838 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642858 59838 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739696 59838 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
118654424 189593 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5174211 189593 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
162676953 182940 0 None 39 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4799851 182940 0 None 39 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 453 4 1 7 3.4 O=S(=O)(c1cccc(Cl)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
10027518 159116 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103877 159116 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
56595667 65320 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834241 65320 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 326 4 1 3 1.8 CCN/C(=N\S(=O)(=O)c1cccc(F)c1)N1CC(CC)C=N1 10.1021/jm200466r
135398737 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
38 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
722 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
CHEMBL42 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
DB00363 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2010.07.105
164619216 185082 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185082 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
135398737 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
38 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
722 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
CHEMBL42 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
DB00363 944 89 None -4 91 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2011657
16718822 182076 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL478894 182076 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
155540721 171926 0 None 213 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4483304 171926 0 None 213 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)[nH]1 10.1016/j.ejmech.2019.06.001
57398615 71205 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71205 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71205 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
66801018 111600 0 None -6 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 502 8 1 7 4.4 Cc1c(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289986 111600 0 None -6 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 502 8 1 7 4.4 Cc1c(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68108559 131109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692851 131109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 4.2 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
68109199 131131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 2 1 5 4.1 O=S(=O)(c1ccc2oc3c(c2c1)C1CCC(C3)N1)n1ccc2ccc(F)cc21 nan
CHEMBL3692872 131131 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 396 2 1 5 4.1 O=S(=O)(c1ccc2oc3c(c2c1)C1CCC(C3)N1)n1ccc2ccc(F)cc21 nan
71451605 83999 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165566 83999 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219894 83999 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 4.0 CNC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
56593647 65353 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834339 65353 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1ccc2ccccc2c1)N1CC(CC)C=N1 10.1021/jm200466r
137636791 155334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4060415 155334 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/acs.jmedchem.6b01662
57393467 69405 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935595 69405 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 371 3 1 5 3.7 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)C(C)(C)NCC4)c1 10.1016/j.bmcl.2011.11.050
129103313 166200 0 None -1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4283548 166200 0 None -1 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 447 6 0 4 5.0 O=C1CCc2cc(CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
56595404 65308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
CHEMBL1834228 65308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCC1C=NN(/C(=N/S(=O)(=O)c2cccc(Cl)c2)NC)C1 10.1021/jm200466r
25263327 191090 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.6 Cc1c(C2CCNCC2)ccnc1OCc1cccc(F)c1 10.1016/j.bmcl.2009.03.077
CHEMBL519670 191090 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 300 4 1 3 3.6 Cc1c(C2CCNCC2)ccnc1OCc1cccc(F)c1 10.1016/j.bmcl.2009.03.077
56595668 65321 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834242 65321 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 2.7 CCN/C(=N\S(=O)(=O)c1cccc(C(F)(F)F)c1)N1CC(CC)C=N1 10.1021/jm200466r
25024146 62628 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCN(C)CC4)ccc32)cc1 10.1021/ml100101u
CHEMBL1785061 62628 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2ccc3cc(CN4CCN(C)CC4)ccc32)cc1 10.1021/ml100101u
25263324 191008 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 343 5 1 2 5.6 CCC(Oc1cccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL519536 191008 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 343 5 1 2 5.6 CCC(Oc1cccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
155567666 175428 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4589391 175428 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
11079889 116965 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 400 6 0 6 2.8 COc1ccc2c(c1)c(CCN1CCOCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL339913 116965 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 400 6 0 6 2.8 COc1ccc2c(c1)c(CCN1CCOCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
134144864 150155 0 None -67 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 600 15 1 7 5.1 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3955917 150155 0 None -67 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 600 15 1 7 5.1 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(OCCN4CCOCC4)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168284197 190262 0 None -141 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 515 12 4 9 3.6 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5184538 190262 0 None -141 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 515 12 4 9 3.6 COc1ccccc1N1CCN(CCCCNc2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
155534362 171338 0 None -81 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 522 8 1 6 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccccc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
CHEMBL4469813 171338 0 None -81 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 522 8 1 6 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccccc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
168274231 189873 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5178803 189873 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 3 1 4 4.9 OC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
57396417 71203 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949975 71203 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1963009 71203 0 None -81 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 484 5 0 5 4.1 O=S(=O)(c1ccc2cccnc2c1)N1CCC(CN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
135449090 188725 3 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL512332 188725 3 None 2 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 268 1 1 2 1.9 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccccc23)N1C 10.1016/j.bmc.2013.09.011
44393045 161110 0 None -87 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 370 7 3 6 3.6 C[C@H](Nc1nc(N)nc(NCCc2ccc(F)cc2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
CHEMBL413049 161110 0 None -87 3 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 370 7 3 6 3.6 C[C@H](Nc1nc(N)nc(NCCc2ccc(F)cc2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
11667340 154147 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 344 5 1 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(F)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL399681 154147 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 344 5 1 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(F)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
134151980 152656 0 None -109 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 570 14 1 6 5.1 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3977072 152656 0 None -109 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 570 14 1 6 5.1 O=C(CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(OCCN2CCOCC2)cc1 10.1016/j.ejmech.2016.05.005
57396855 71130 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949969 71130 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1962400 71130 0 None -4 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.12.039
155551114 176096 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4541606 176096 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598210 176096 0 None -26 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 431 8 0 3 5.3 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
168279281 190428 0 None -309 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 342 7 3 8 1.1 Nc1nc(N)nc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5186821 190428 0 None -309 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 342 7 3 8 1.1 Nc1nc(N)nc(NCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
24839550 136791 14 None -28 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752576 136791 14 None -28 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 240 7 1 1 3.4 C=CCN(CC=C)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2015.12.053
25263315 172661 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 306 4 1 3 3.9 Cc1c(OCc2cccc(C#N)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL452402 172661 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 306 4 1 3 3.9 Cc1c(OCc2cccc(C#N)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
57393365 71206 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None -9 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
168287395 190847 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 377 4 1 4 5.1 Clc1cccc(Cn2ccc3c(N[C@H]4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5193046 190847 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 377 4 1 4 5.1 Clc1cccc(Cn2ccc3c(N[C@H]4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
162664825 181507 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CC(F)(F)F)CC3)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4781626 181507 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CC(F)(F)F)CC3)cccc21 10.1016/j.ejmech.2020.112916
1355 1980 82 None -125 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
142 1980 82 None -125 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
CHEMBL478 1980 82 None -125 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
DB12110 1980 82 None -125 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1016/j.ejmech.2022.114319
49781252 17003 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 744 14 2 9 5.8 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256257 17003 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 744 14 2 9 5.8 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
155546176 172953 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2cc(C3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4531106 172953 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2cc(C3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
145983760 164988 0 None -17 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241497 164988 0 None -17 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44591028 176214 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 5 0 6 4.6 CC(C)CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL460624 176214 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 5 0 6 4.6 CC(C)CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
71460468 81013 0 None -58 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 403 7 1 4 4.2 CC(C)c1ccccc1OCCN1CCC(NC(=O)c2ccc3ccccc3n2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159468 81013 0 None -58 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 403 7 1 4 4.2 CC(C)c1ccccc1OCCN1CCC(NC(=O)c2ccc3ccccc3n2)C1 10.1016/j.ejmech.2012.07.043
90654852 112139 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233675 112139 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302762 112139 0 None -38 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
71454998 81005 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 450 9 1 4 4.5 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159460 81005 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 450 9 1 4 4.5 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2012.07.043
126720448 161987 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4167974 161987 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
44352308 116984 0 None -218 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 116984 0 None -218 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor using [3H]LSD as radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
71458649 81018 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 370 7 1 5 2.3 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159473 81018 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 370 7 1 5 2.3 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
162661003 180816 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccccc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4763575 180816 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccccc3)cc21 10.1016/j.ejmech.2020.112916
168291978 191415 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 482 6 3 7 4.2 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5201719 191415 0 None -1 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 482 6 3 7 4.2 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
71453278 81012 0 None -117 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 7 1 3 4.5 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccc(F)c1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159467 81012 0 None -117 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 7 1 3 4.5 O=C(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccc(F)c1F 10.1016/j.ejmech.2012.07.043
69939760 127406 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1ccc2c(ccn2S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664752 127406 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 6 3.7 COc1ccc2c(ccn2S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258791 128469 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128469 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
9905247 106765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL316881 106765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
44389091 121506 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL359460 121506 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 368 4 1 5 3.3 COc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
10246789 170441 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1c(S(=O)(=O)c2ccccc2)c2ccccc2n1CCN(C)C 10.1016/j.bmcl.2004.09.003
CHEMBL445652 170441 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1c(S(=O)(=O)c2ccccc2)c2ccccc2n1CCN(C)C 10.1016/j.bmcl.2004.09.003
9905247 106765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm030030n
CHEMBL316881 106765 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm030030n
2105 3005 34 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3005 34 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3005 34 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3005 34 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3005 34 None -19 33 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
44567984 188631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL511489 188631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccc(Cl)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
155514839 169319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4440598 169319 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
155519088 169772 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4447200 169772 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
145985527 165156 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245622 165156 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
90469118 183877 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1ccc(F)c(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4846691 183877 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1ccc(F)c(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469116 183951 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1ccc(F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4847804 183951 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1ccc(F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
155567905 175422 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 566 12 1 5 7.5 Cc1c(OCc2ccccc2)cccc1N1CCN(CCCCCCNc2c3c(nc4c2CCCC4)CCCC3)CC1 10.1016/j.ejmech.2019.07.040
CHEMBL4589118 175422 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 566 12 1 5 7.5 Cc1c(OCc2ccccc2)cccc1N1CCN(CCCCCCNc2c3c(nc4c2CCCC4)CCCC3)CC1 10.1016/j.ejmech.2019.07.040
57400391 69408 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935598 69408 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 389 4 1 5 3.4 COCC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
46880656 5946 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cccc(F)c12 10.1016/j.bmcl.2010.01.073
CHEMBL1080331 5946 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cccc(F)c12 10.1016/j.bmcl.2010.01.073
46880659 6304 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(F)ccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082200 6304 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(F)ccc12 10.1016/j.bmcl.2010.01.073
25024530 62631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1785064 62631 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
16718919 198099 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
CHEMBL593889 198099 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 1 6 4.5 CC1=C(C2CCCN(C)C2)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
155569337 175557 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 410 5 2 6 3.2 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4592085 175557 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 410 5 2 6 3.2 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
24771185 183553 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 2 6 3.8 O=S(=O)(c1cccc2ccccc12)n1ncc2ccc(NCC3CCNCC3)cc21 10.1016/j.bmcl.2009.03.071
CHEMBL482756 183553 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 2 6 3.8 O=S(=O)(c1cccc2ccccc12)n1ncc2ccc(NCC3CCNCC3)cc21 10.1016/j.bmcl.2009.03.071
56943599 111594 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289980 111594 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
68109169 131132 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3cc(S(=O)(=O)c4ccccc4)ccc3c2C1 nan
CHEMBL3692873 131132 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3cc(S(=O)(=O)c4ccccc4)ccc3c2C1 nan
68115778 131725 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696960 131725 0 None - 1 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2ccc(F)cc2)cc2c3c(oc12)CCNC3 nan
16222758 81639 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 3 0 4 4.3 Cc1ccc(S(=O)(=O)n2c3c(c4cc(Cl)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165554 81639 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 3 0 4 4.3 Cc1ccc(S(=O)(=O)n2c3c(c4cc(Cl)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
25123011 199508 0 None 74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
CHEMBL603483 199508 0 None 74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc5ccccc5c4)c3c2)CC1 10.1021/jm901674f
10094169 156242 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(OC)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4070850 156242 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(OC)ccc32)cc1 10.1021/acs.jmedchem.6b01662
137652249 156570 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4074732 156570 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1cccc2c1c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
25263346 183509 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482541 183509 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 4 3.4 Cc1c(OS(=O)(=O)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
11282389 60497 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 7 2.6 CN(C)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
CHEMBL176218 60497 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 5 2 7 2.6 CN(C)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
58158682 138438 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785259 138438 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1cccc(O)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
56595666 65319 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834240 65319 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccc(Cl)cc1)N1CC(CC)C=N1 10.1021/jm200466r
11362134 62856 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL179006 62856 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 1 4 4.7 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
137643300 157865 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 4 1 6 3.1 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090177 157865 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 463 4 1 6 3.1 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
1150 3817 116 None -7 24 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
125 3817 116 None -7 24 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
CHEMBL6640 3817 116 None -7 24 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
DB08653 3817 116 None -7 24 Human 6.8 pKi = 6.8 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm990550b
44327952 206304 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 206304 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
66801624 155961 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 6 2 3 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4067700 155961 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 6 2 3 5.4 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
56944953 159107 0 None -66 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4103725 159107 0 None -66 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
145971527 162567 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 337 7 1 2 5.6 Cc1ccc(C(C)NCCC(c2ccc(F)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4177293 162567 0 None 3 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 337 7 1 2 5.6 Cc1ccc(C(C)NCCC(c2ccc(F)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
24854106 160514 1 None -89 8 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
CHEMBL411663 160514 1 None -89 8 Human 5.8 pKi = 5.8 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
53327979 111205 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286589 111205 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
145985958 165058 0 None -151 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4243036 165058 0 None -151 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
155562834 174634 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 450 8 0 5 4.1 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4571077 174634 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 450 8 0 5 4.1 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
137655693 158316 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 285 3 1 7 0.2 CN1CCN(c2nc(N)nc(Cc3ccncc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4094953 158316 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 285 3 1 7 0.2 CN1CCN(c2nc(N)nc(Cc3ccncc3)n2)CC1 10.1016/j.ejmech.2017.04.033
12017576 102505 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL306569 102505 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)c1 10.1016/s0960-894x(00)00453-4
57402187 69407 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935597 69407 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 395 3 1 4 4.0 CC1(C(F)F)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
155519102 169787 0 None 9 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4447416 169787 0 None 9 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164619075 185601 0 None -114 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 413 7 0 5 2.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4872713 185601 0 None -114 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 413 7 0 5 2.8 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
145961372 161059 0 None -83 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4129589 161059 0 None -83 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 311 7 0 2 5.3 c1ccc2c(OCCCCCN3CCCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
53327979 111205 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286589 111205 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 387 2 1 5 2.9 O=S(=O)(c1ccc(Cl)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
10563312 202966 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1016/j.bmcl.2004.05.076
CHEMBL7379 202966 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1016/j.bmcl.2004.05.076
10563312 202966 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1021/jm990550b
CHEMBL7379 202966 2 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 1 2 3.2 CCCc1[nH]c2ccc(OC)cc2c1CCN(C)C 10.1021/jm990550b
59511191 184941 3 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4862745 184941 3 None -2 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 228 2 2 3 1.5 c1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
71451458 81031 0 None -37 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 5 3.5 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159486 81031 0 None -37 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 5 3.5 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
4725280 172639 4 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 2 2 5.4 Clc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4522860 172639 4 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 2 2 5.4 Clc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155540541 171945 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4483496 171945 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2ccc(N3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
24829343 158475 0 None -234 9 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 158475 0 None -234 9 Human 6.7 pKi = 6.7 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
155569022 175862 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4592962 175862 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596261 175862 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
3561 18886 34 None -3 11 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 18886 34 None -3 11 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
137642134 157796 0 None -131 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4089427 157796 0 None -131 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccc(F)cc3)CC2)CC1 10.1016/j.bmc.2017.04.046
73350823 102057 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102057 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102057 0 None -12 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptor by competitive binding assayBinding affinity to human 5HT6 receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
44443511 153927 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 339 5 1 5 2.8 COC(=O)c1cc(N2CCN(C)CC2)ccc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL399024 153927 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 339 5 1 5 2.8 COC(=O)c1cc(N2CCN(C)CC2)ccc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
156011936 176828 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 8 1 6 4.3 O=c1[nH]c2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4638308 176828 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 8 1 6 4.3 O=c1[nH]c2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
156019026 177222 0 None -38 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 7 4.6 O=c1oc2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4643450 177222 0 None -38 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 7 4.6 O=c1oc2ccccc2n1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
44389023 62186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
CHEMBL178193 62186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2004.10.064
9841077 9398 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL112024 9398 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
107715 199260 18 None -29 20 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199260 18 None -29 20 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199260 18 None -29 20 Human 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
44567982 178435 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL471099 178435 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1ccccc1Cl)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
24894055 182586 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL479548 182586 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccccc1S(=O)(=O)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
44568062 190061 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 370 3 0 5 2.9 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL518153 190061 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 370 3 0 5 2.9 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C)CC3)c1 10.1016/j.bmcl.2008.06.030
44389023 62186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL178193 62186 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 418 4 1 5 4.4 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/acsmedchemlett.6b00056
155539600 172290 0 None 21 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 7 2.7 CC(Sc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4515075 172290 0 None 21 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 7 2.7 CC(Sc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
137660291 158861 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4100818 158861 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
11632439 93568 6 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL248658 93568 6 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
53259021 69404 0 None -6 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69404 0 None -6 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
155540796 175782 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4516784 175782 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4595674 175782 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 396 5 2 6 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
24763352 62294 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783601 62294 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 389 3 1 4 3.9 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(Cl)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
57414390 131099 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692841 131099 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCC3 nan
68108422 131151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 4 2 5 2.8 CC(O)Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692892 131151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 4 2 5 2.8 CC(O)Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
68108636 131152 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131152 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115647 131182 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 443 4 0 4 5.2 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCC(F)(F)F)CC3 nan
CHEMBL3692923 131182 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 443 4 0 4 5.2 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(CCC(F)(F)F)CC3 nan
162662399 181347 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4779739 181347 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
25263328 183710 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.5 Cc1c(C2CCNCC2)ccnc1OCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484010 183710 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.5 Cc1c(C2CCNCC2)ccnc1OCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2009.03.077
44403100 71652 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 384 5 0 5 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL197407 71652 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 384 5 0 5 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL5080305 212905 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1cccc(S(=O)(=O)CC2CCN(CCCc3noc4cc(F)ccc34)C2)c1 10.1021/acs.jmedchem.1c00497
25263344 183569 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 3.2 Cc1c(OS(=O)(=O)c2ccccc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482939 183569 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 331 4 1 4 3.2 Cc1c(OS(=O)(=O)c2ccccc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
16222867 81184 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 5 0 6 3.3 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2163369 81184 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 414 5 0 6 3.3 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
11176859 62975 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm049615n
CHEMBL179344 62975 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm049615n
17940080 46762 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 2 7 2.1 COc1ccc(S(=O)(=O)Nc2cc([N+](=O)[O-])ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154186 46762 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 2 7 2.1 COc1ccc(S(=O)(=O)Nc2cc([N+](=O)[O-])ccc2C)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9914461 205958 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 514 5 2 6 5.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C(C)C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95504 205958 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 514 5 2 6 5.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@H](C(C)C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
11064294 67611 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 2 3 1.8 CCOC(=O)c1[nH]c2ccccc2c1CCN 10.1021/jm050247c
CHEMBL191121 67611 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 2 3 1.8 CCOC(=O)c1[nH]c2ccccc2c1CCN 10.1021/jm050247c
44390105 11643 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1181578 11643 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL181877 11643 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
145985289 165154 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cncc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245607 165154 0 None -31 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 534 6 0 6 5.6 O=S(=O)(c1cncc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
44393574 123517 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 189 3 0 1 1.5 CN(C)CC[N+]1=CCc2ccccc21 10.1016/j.bmcl.2004.05.076
CHEMBL363035 123517 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 189 3 0 1 1.5 CN(C)CC[N+]1=CCc2ccccc21 10.1016/j.bmcl.2004.05.076
2962174 162421 10 None 44 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 410 5 1 4 4.2 O=C1N(Cc2ccccc2)C(c2ccccc2)=NC1(Nc1ccccn1)C(F)(F)F 10.1016/j.ejmech.2018.04.010
CHEMBL4174981 162421 10 None 44 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 410 5 1 4 4.2 O=C1N(Cc2ccccc2)C(c2ccccc2)=NC1(Nc1ccccn1)C(F)(F)F 10.1016/j.ejmech.2018.04.010
90656173 110355 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1ccc(N2CCNCC2)cc1 10.1016/j.bmcl.2014.03.049
CHEMBL3260806 110355 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 357 3 1 4 3.4 O=C1OC(c2ccccc2Cl)CN1c1ccc(N2CCNCC2)cc1 10.1016/j.bmcl.2014.03.049
13069598 120103 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360998 120103 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546116 120103 0 None -26 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
71727066 90834 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401936 90834 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3215930 90834 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 338 3 0 5 2.7 COc1ccc2c(=O)c3cc(CN4CCN(C)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
155567307 175369 0 None -173 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 457 10 0 4 5.6 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4587772 175369 0 None -173 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 457 10 0 4 5.6 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc2c34)CC1 10.1016/j.bmcl.2019.06.029
57394332 70422 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950767 70422 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57399092 68092 0 None -75 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 468 9 0 6 3.5 CCN(CCCN1CCN(c2ccccc2OC)CC1)S(=O)(=O)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917355 68092 0 None -75 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 468 9 0 6 3.5 CCN(CCCN1CCN(c2ccccc2OC)CC1)S(=O)(=O)c1ccc2ncccc2c1 10.1016/j.bmc.2011.09.044
57394332 70422 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950767 70422 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 353 2 1 5 2.8 Cn1c2c(c3cc(S(=O)(=O)c4ccccn4)ccc31)C1CCC(C2)N1 nan
44567932 191472 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL520267 191472 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.6 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
137657740 159099 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
CHEMBL4103656 159099 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
417052 116355 37 None -2 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1016/j.bmcl.2003.09.027
CHEMBL338115 116355 37 None -2 3 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 214 1 1 2 2.5 COc1ccc2[nH]c3c(c2c1)CCN=C3C 10.1016/j.bmcl.2003.09.027
137658350 159259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 493 5 0 6 4.1 CSc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4105632 159259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 493 5 0 6 4.1 CSc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
49781469 17005 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 800 18 2 9 7.4 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256259 17005 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 800 18 2 9 7.4 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
11282295 62957 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 8 1 4 4.9 O=S(=O)(CCc1cccc2ccccc12)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm049615n
CHEMBL179264 62957 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 8 1 4 4.9 O=S(=O)(CCc1cccc2ccccc12)Nc1ccc2ccn(CCN3CCCC3)c2c1 10.1021/jm049615n
168291617 191437 0 None -123 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 413 8 0 6 3.5 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5202054 191437 0 None -123 5 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 413 8 0 6 3.5 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
90654846 112199 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233672 112199 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304317 112199 0 None -43 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.01.065
71726944 101931 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3039669 101931 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3215698 101931 0 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 342 2 0 4 3.3 CN1CCN(Cc2cccc3c(=O)c4ccc(Cl)cc4oc23)CC1 10.1016/j.bmcl.2013.05.062
162667511 181917 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 554 12 0 5 6.4 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4786924 181917 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 554 12 0 5 6.4 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1 10.1016/j.ejmech.2020.112765
54764323 68096 0 None -151 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
CHEMBL1917359 68096 0 None -151 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 429 8 0 4 4.5 CCN(CCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
1548955 88153 17 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
2800 88153 17 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
CHEMBL2355051 88153 17 None -20 18 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
24783296 176044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2nc(N3CCNCC3)oc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
CHEMBL459782 176044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2nc(N3CCNCC3)oc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
56593644 65350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834336 65350 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1c(Cl)cccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
11567716 94240 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 1 1 2 4.3 CC1(c2ccccc2)C(=O)Nc2cc(Br)cc(Br)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL252673 94240 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 1 1 2 4.3 CC1(c2ccccc2)C(=O)Nc2cc(Br)cc(Br)c2C1=O 10.1016/j.bmcl.2007.11.045
12017580 206210 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1016/j.bmcl.2004.05.076
CHEMBL97017 206210 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1016/j.bmcl.2004.05.076
12017580 206210 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1021/jm030030n
CHEMBL97017 206210 1 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1cccc2c(CCN(C)C)c[nH]c12 10.1021/jm030030n
21557475 174317 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 442 8 0 5 4.2 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4564093 174317 0 None -11 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 442 8 0 5 4.2 O=C1c2cccc3cccc(c23)C(=O)N1CCCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2019.06.029
164618510 185351 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 4.1 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4869198 185351 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 481 7 0 5 4.1 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
13069611 120099 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3360995 120099 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546110 120099 0 None -1621 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 426 7 0 9 1.0 COc1ccccc1N1CCN(CCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
675366 171222 11 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 1 0 5 2.6 Cc1nc(N2CCCN(C)CC2)c2c3c(sc2n1)CCC3 10.1016/j.ejmech.2019.111857
CHEMBL4467920 171222 11 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 302 1 0 5 2.6 Cc1nc(N2CCCN(C)CC2)c2c3c(sc2n1)CCC3 10.1016/j.ejmech.2019.111857
156015087 176966 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 406 7 1 4 4.8 C=CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640150 176966 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 406 7 1 4 4.8 C=CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
20923078 117432 5 None 1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 4 2 5 3.2 O=c1ccc(-c2ccc(S(=O)(=O)Nc3cccc4c3CCCC4)s2)n[nH]1 10.1016/j.bmcl.2015.03.049
CHEMBL3403339 117432 5 None 1 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 4 2 5 3.2 O=c1ccc(-c2ccc(S(=O)(=O)Nc3cccc4c3CCCC4)s2)n[nH]1 10.1016/j.bmcl.2015.03.049
71455000 81011 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159466 81011 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155527191 170600 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 2 4 4.8 COc1ccc2[nH]cc(CCN(C)Cc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4458840 170600 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 2 4 4.8 COc1ccc2[nH]cc(CCN(C)Cc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
71455000 81011 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1039/C5MD00166H
CHEMBL2159466 81011 0 None -28 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 472 8 1 4 4.5 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)c(F)c1 10.1039/C5MD00166H
134150900 151419 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3966484 151419 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@@H]1CCO 10.1016/j.bmc.2016.10.010
242 467 117 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 467 117 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 467 117 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 467 117 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 467 117 None -144 51 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
22557224 93075 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 452 5 2 7 1.1 CS(=O)(=O)Nc1cccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cccc32)c1 10.1016/j.bmcl.2006.12.093
CHEMBL246289 93075 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 452 5 2 7 1.1 CS(=O)(=O)Nc1cccc(S(=O)(=O)N2CCOc3c(N4CCNCC4)cccc32)c1 10.1016/j.bmcl.2006.12.093
164614734 184814 0 None -660 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 443 8 0 6 2.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4860754 184814 0 None -660 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 443 8 0 6 2.8 COc1ccccc1N1CCN(CCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
10257042 202658 0 None -50 7 Human 5.7 pKi = 5.7 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 202658 0 None -50 7 Human 5.7 pKi = 5.7 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
44386717 60096 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 413 5 1 6 3.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL175068 60096 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 413 5 1 6 3.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(N)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
67085077 127393 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(NC5CCCC5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664739 127393 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 5 4.7 Cn1c2c(c3cc(S(=O)(=O)c4cccc(NC5CCCC5)c4)ccc31)C1CCC(C2)N1 nan
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
44389081 62324 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178385 62324 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 373 3 2 5 3.1 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3cc(F)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44388999 63051 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179592 63051 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
11739679 169285 0 None 776 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL444015 169285 0 None 776 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 353 3 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccccc32)cc1 10.1016/j.bmcl.2004.10.064
9950402 169886 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL444878 169886 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 352 3 0 4 3.6 CN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.05.092
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.05.092
118879893 160656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
CHEMBL4080401 160656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
CHEMBL4117763 160656 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 463 5 1 6 3.1 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccccc1Br 10.1016/j.bmcl.2021.128275
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmc.2009.08.006
9902533 133079 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
CHEMBL371292 133079 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmc.2009.08.006
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.08.006
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmc.2009.08.006
23844114 205784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
23844114 205784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1021/jm030030n
CHEMBL94569 205784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL94569 205784 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 373 6 1 6 2.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(N)cc1 10.1021/jm030030n
155519559 169813 0 None 15 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4447846 169813 0 None 15 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
155512487 169102 2 None 5 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4437523 169102 2 None 5 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
155565813 175235 0 None 47 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4cc(F)ccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4584504 175235 0 None 47 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 350 6 3 3 4.6 Oc1ccc(-c2ccc(CNCCc3c[nH]c4cc(F)ccc34)o2)cc1 10.1016/j.ejmech.2019.111857
90469381 184815 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4860809 184815 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 424 3 0 6 3.3 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.1c00224
90469319 185106 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 0 6 3.2 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4865309 185106 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 0 6 3.2 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1021/acs.jmedchem.1c00224
90469380 185591 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 440 3 0 6 3.8 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4872586 185591 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 440 3 0 6 3.8 CN1CCN(c2nc3ccccc3c3c2ccn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.1c00224
164617683 183931 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4847532 183931 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113783
164615023 184209 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 494 12 2 8 3.5 O=[N+]([O-])c1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
CHEMBL4851595 184209 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 494 12 2 8 3.5 O=[N+]([O-])c1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
164620015 185044 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 11 2 6 3.9 Cc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
CHEMBL4864206 185044 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 11 2 6 3.9 Cc1cccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113783
126720436 180171 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 385 4 1 7 2.2 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
CHEMBL4756098 180171 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 385 4 1 7 2.2 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.0c02009
162644347 181177 0 None 158 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4777550 181177 0 None 158 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 377 3 1 7 1.7 O=S(=O)(c1cccc(Cl)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
134130920 141682 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 571 10 1 7 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884195 141682 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 571 10 1 7 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130564 141684 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 12 1 6 5.4 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884227 141684 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 530 12 1 6 5.4 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134131252 141760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 621 11 1 7 7.1 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3885186 141760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 621 11 1 7 7.1 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
10073773 160576 13 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4082473 160576 13 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4117187 160576 13 None 309 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 477 5 0 6 3.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137631027 160598 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4101284 160598 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117309 160598 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 455 6 0 6 4.1 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44388999 63051 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL179592 63051 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
9924959 69121 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL193358 69121 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 3 0 4 3.4 CN1CCC(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
10270799 71428 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 4.0 O=S(=O)(c1cccc(Cl)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196692 71428 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 4.0 O=S(=O)(c1cccc(Cl)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
9902533 133079 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133079 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44433197 88347 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236313 88347 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 437 3 1 8 2.8 CN1CCCC(n2cc(S(=O)(=O)C3=C(Cl)NC4SC=CN34)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44435603 91318 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL240922 91318 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccccc1F)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
44435640 154390 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL401019 154390 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1ccccc1F)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm8009469
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm8009469
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm8009469
155510928 175895 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4435010 175895 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4596543 175895 0 None 398 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 368 4 2 6 2.9 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm070521y
127047901 139103 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 442 6 0 7 3.3 COc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
CHEMBL3797651 139103 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 442 6 0 7 3.3 COc1ccc(-c2cc(N3CCN(C)CC3)nc3c2ccn3S(=O)(=O)CC(C)C)cc1 10.1016/j.bmcl.2016.04.024
10472158 195150 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565745 195150 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/jm900796p
49836924 18586 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
CHEMBL1278000 18586 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 496 5 0 6 4.8 CN1CCN(c2ccc3c(c2)c(S(=O)(=O)c2cccc4ccccc24)nn3Cc2ccccc2)CC1 10.1021/jm1007825
57400234 71196 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71196 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71196 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1021/acs.jmedchem.5b00179
44155874 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
CHEMBL1668500 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2011.01.038
11463428 200067 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606639 200067 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
11282884 200610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
CHEMBL610256 200610 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 473 5 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049243i
68108768 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1cccc(C2CCOC2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692883 131142 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1cccc(C2CCOC2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115758 131716 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696951 131716 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 3.5 Cc1cc(S(=O)(=O)c2ccc(F)c(F)c2)cc2c3c(oc12)CCNC3 nan
162664339 181546 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4782149 181546 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1csc2ccccc12 10.1016/j.ejmech.2020.112149
44435638 154389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL401018 154389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
52913108 70417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70417 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.01.031
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1007/s00044-004-0121-8
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1007/s00044-004-0121-8
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.05.106
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.05.106
45113400 14116 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1099284 14116 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199172 14116 2 None 3 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 359 3 2 3 3.1 CN1CCc2[nH]c3ccc(S(=O)(=O)Nc4cccc(F)c4)cc3c2C1 10.1016/j.ejmech.2009.10.035
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
44435638 154389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL401018 154389 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.2 CN1CCCC(n2cc(S(=O)(=O)c3cccc(C(F)(F)F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57393468 69409 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935599 69409 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOCC1)NCC3 10.1016/j.bmcl.2011.11.050
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.7b00085
6918542 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070910s
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.7b00085
CHEMBL76237 203216 20 None 11 10 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070910s
45484383 195143 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565731 195143 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2ccccc2C(F)(F)F)c2cccnc21 10.1016/j.bmc.2009.05.055
45484384 197189 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584049 197189 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 2.8 NCCn1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263301 184036 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
CHEMBL484927 184036 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 1 6 4.1 CCN(CC)CCC(=O)Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmcl.2009.03.071
44155874 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of 5-HT6 receptor (unknown origin)Inhibition of 5-HT6 receptor (unknown origin)
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00056
CHEMBL1668500 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of 5-HT6 receptor (unknown origin)Inhibition of 5-HT6 receptor (unknown origin)
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00056
68109346 131134 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3692875 131134 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c3c(oc2c1)CCNC3 nan
68115761 131722 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1ccccc1)c1cc(C(F)(F)F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696957 131722 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 381 2 1 4 3.9 O=S(=O)(c1ccccc1)c1cc(C(F)(F)F)c2oc3c(c2c1)CNCC3 nan
10026658 155760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4065437 155760 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44476701 126899 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659968 126899 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 328 2 1 6 1.5 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
44155874 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
CHEMBL1668500 57315 15 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 333 3 0 6 2.9 CSc1nn2c(C)cc(C)nc2c1S(=O)(=O)c1ccccc1 nan
44435618 88354 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236334 88354 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 10.1016/j.bmcl.2021.128275
10202564 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
10202564 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
3217 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
3217 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
CHEMBL362628 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.bmc.2009.08.006
CHEMBL362628 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm900796p
44435618 88354 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236334 88354 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccccc3Cl)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
10202564 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
3217 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
CHEMBL362628 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm8009469
44554228 18555 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277752 18555 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 5 1 6 3.8 CCCn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
45483622 196414 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574403 196414 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 449 4 3 9 2.0 O=S(=O)(Nc1ccc2c(c1)/C(=N/NC1=NCCN1)CC2)c1c(Cl)nc2sccn12 10.1021/jm900796p
10202564 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
3217 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
CHEMBL362628 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1021/jm049615n
68115604 131171 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1cccc(-n2cccn2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692912 131171 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1cccc(-n2cccn2)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
118010062 131181 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 5 4.2 O=S(=O)(c1ccc(OC(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692922 131181 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 5 4.2 O=S(=O)(c1ccc(OC(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115807 131246 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2ccc(C3CCOC3)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692987 131246 0 None - 1 Human 8.7 pKi = 8.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 4 1 6 3.4 COc1cc(S(=O)(=O)c2ccc(C3CCOC3)cc2)cc2c3c(oc12)CCNC3 nan
11024311 88215 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 341 3 2 5 2.3 CNc1cc(S(=O)(=O)c2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
CHEMBL23575 88215 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 341 3 2 5 2.3 CNc1cc(S(=O)(=O)c2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
9822215 205381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL92093 205381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
18180040 67697 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2ccc(I)cc2)cc1N1CCNCC1 10.1021/jm5003952
CHEMBL191429 67697 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 473 5 2 5 2.5 COc1ccc(NS(=O)(=O)c2ccc(I)cc2)cc1N1CCNCC1 10.1021/jm5003952
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm5003952
58258779 128463 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 398 3 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(O)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669662 128463 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 398 3 2 6 3.1 COc1cc(S(=O)(=O)c2cccc(O)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
10069592 125832 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 400 8 0 5 3.9 CCCc1c(CCN(C)C)c2cc(OC)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
CHEMBL365040 125832 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 400 8 0 5 3.9 CCCc1c(CCN(C)C)c2cc(OC)ccc2n1S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2004.05.076
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2012.06.002
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2012.06.002
9822215 205381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2012.06.002
CHEMBL92093 205381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 398 5 0 5 3.9 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2012.06.002
16019580 10463 2 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1169707 10463 2 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 435 5 0 8 3.8 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
16117152 59770 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642885 59770 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739101 59770 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1ccc(Cl)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.07.028
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2009.04.108
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070521y
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2009.04.108
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm070521y
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2007.11.045
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2007.11.045
10067306 197188 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL584046 197188 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
24771120 183518 0 None 56 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
CHEMBL482562 183518 0 None 56 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCNCC1 10.1016/j.bmcl.2009.03.071
155554569 173642 0 None 245 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4548434 173642 0 None 245 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
71151704 117753 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 544 8 1 7 4.4 O=C1CCc2ccc(OCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409254 117753 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 544 8 1 7 4.4 O=C1CCc2ccc(OCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.5b00179
68115760 131193 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.4 O=S(=O)(c1cc(F)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692934 131193 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.4 O=S(=O)(c1cc(F)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23625764 146772 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL392899 146772 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44126269 199799 4 None -6 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
CHEMBL605081 199799 4 None -6 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 318 3 0 2 4.5 Cc1ccc(CCn2c3c(c4cc(C)ccc42)CN(C)CC3)cc1 10.1016/j.bmcl.2009.11.037
44387089 128285 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 524 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(I)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL366935 128285 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 524 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(I)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44389025 122613 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL361189 122613 0 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
58258798 128485 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669684 128485 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 3 1 6 3.9 COc1cc(S(=O)(=O)c2cn(C)c3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258802 128492 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
CHEMBL3669691 128492 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 446 3 1 6 4.3 [C-]#[N+]c1ccc2ccn(S(=O)(=O)c3cc(OC)c4c(c3)c3c(n4C)CC4CCC3N4)c2c1 nan
44389025 122613 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361189 122613 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
9817810 17190 1 None 1 8 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 17190 1 None 1 8 Human 8.6 pKi = 8.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
23625764 146772 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL392899 146772 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 1 5 2.9 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
52913108 70417 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70417 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
25263339 183587 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 384 4 1 3 5.2 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(Cl)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
CHEMBL482989 183587 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 384 4 1 3 5.2 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(Cl)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
56944666 111621 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290006 111621 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
56943600 111623 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 8 1 5 5.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3290008 111623 0 None -3 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 8 1 5 5.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
68115749 131747 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 131747 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
44438719 93458 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL248071 93458 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
44435614 153913 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL399013 153913 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
137635355 155715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 300 4 1 4 2.4 NCCc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1021/acs.jmedchem.7b00085
CHEMBL4064950 155715 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 300 4 1 4 2.4 NCCc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1 10.1021/acs.jmedchem.7b00085
25263313 172162 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(OCc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL450673 172162 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(OCc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
68115727 131174 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)CCOC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692915 131174 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)CCOC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
17940228 47189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2ccc(Cl)c(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154525 47189 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 415 5 2 5 3.2 COc1ccc(S(=O)(=O)Nc2ccc(Cl)c(Cl)c2)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354574 47322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 581 5 2 5 4.2 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154641 47322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 581 5 2 5 4.2 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369858 47408 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154720 47408 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369855 119307 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL348364 119307 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Br)c2F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9805455 206368 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cnc2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc2c1N1CCNCC1 10.1016/s0960-894x(01)00558-3
CHEMBL97899 206368 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 2 6 4.9 Cc1cnc2ccc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)cc2c1N1CCNCC1 10.1016/s0960-894x(01)00558-3
3232 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
3248571 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
CHEMBL60264 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm980532e
3232 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
3248571 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
CHEMBL60264 3453 13 None 2 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10.1021/jm050247c
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm050247c
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm050247c
6918479 56367 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.12.007
CHEMBL1642114 56367 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 429 4 1 8 2.2 CSc1nn2c(N3CCNCC3)c3c(nc2c1S(=O)(=O)c1ccccc1)CCC3 10.1016/j.bmcl.2010.12.007
44435614 153913 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL399013 153913 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 0 5 2.7 CN1CCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
6918542 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.12.007
CHEMBL76237 203216 20 None 11 10 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2010.12.007
46890158 6381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 4 1 3 3.4 CN(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1082510 6381 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 390 4 1 3 3.4 CN(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
9822810 69159 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL193400 69159 0 None 6 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10293741 71611 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.1 Cn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c21 10.1016/j.bmcl.2005.06.107
CHEMBL197297 71611 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 3 1 5 3.1 Cn1cc(S(=O)(=O)c2cccc(Cl)c2)c2cccc(N3CCNCC3)c21 10.1016/j.bmcl.2005.06.107
22557287 149049 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 3 1 5 2.0 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL394689 149049 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 373 3 1 5 2.0 Cc1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1)CCO2 10.1016/j.bmcl.2006.12.093
25024930 62635 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785068 62635 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
24856058 62604 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 461 5 0 5 3.8 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
CHEMBL1784916 62604 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 461 5 0 5 3.8 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
162643812 181081 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
CHEMBL4776225 181081 0 None -2 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc2ccccc12 10.1016/j.ejmech.2020.112149
25024924 62637 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 5 3.1 O=S(=O)(c1ccc(F)cc1)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785070 62637 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 4 1 5 3.1 O=S(=O)(c1ccc(F)cc1)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
3235 3464 12 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
6918553 3464 12 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
CHEMBL329383 3464 12 None - 1 Human 8.6 pKi = 8.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm5003952
58258867 127400 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 428 3 1 4 5.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664746 127400 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 428 3 1 4 5.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccccc5)c4)ccc31)C1CCC(C2)N1 nan
44389529 130814 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 406 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL368698 130814 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 406 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
49836716 18476 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1277011 18476 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 424 3 1 5 3.5 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4c(Cl)cccc4Cl)c3c2)CC1 10.1021/jm1007825
86302554 110344 0 None 1202 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260795 110344 0 None 1202 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
142592111 174679 0 None 61 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.1 CN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4572260 174679 0 None 61 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.1 CN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
44474631 13968 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197618 13968 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL578631 13968 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 423 4 4 7 2.0 N=C(N)N/N=C1\CCc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
16223065 81625 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 434 4 0 5 4.7 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(Cl)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165540 81625 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 434 4 0 5 4.7 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(Cl)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435604 154322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL400627 154322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
52913104 70415 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950760 70415 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258814 128446 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4cc(F)c5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669645 128446 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4cc(F)c5ccccc54)ccc31)C1CCC(C2)N1 nan
56593645 65351 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834337 65351 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 3 2.5 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1F)N1CC(CC)C=N1 10.1021/jm200466r
44435604 154322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL400627 154322 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
57398803 69399 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69399 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69399 0 None 3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
52913104 70415 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950760 70415 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(Cl)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164621197 185667 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 5 3.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4873700 185667 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 5 3.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CC3)cccc21 10.1016/j.ejmech.2021.113792
155555402 173803 0 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4551858 173803 0 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCNCC3)cc21 10.1016/j.bmcl.2016.07.055
25263355 192888 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2ccc3ccccc3c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL527098 192888 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 381 4 1 4 4.4 Cc1c(OS(=O)(=O)c2ccc3ccccc3c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
68115697 131207 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692948 131207 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
7184883 10795 3 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1172725 10795 3 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 411 5 1 9 3.4 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCc1ccco1)c1sccc12 10.1016/j.bmc.2010.05.051
53319441 59783 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642845 59783 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739231 59783 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
56595402 65306 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
46880759 6055 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080899 6055 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 0 5 3.9 CN1CCC(n2cc(S(=O)(=O)c3cccc4cccnc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
71151757 117756 0 None 27 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 532 10 1 7 4.0 NC(=O)c1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409257 117756 0 None 27 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 532 10 1 7 4.0 NC(=O)c1ccccc1OCCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
25263322 183726 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484164 183726 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL5077755 212742 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.1c00497
68544798 84102 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL2220317 84102 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL3215892 84102 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
71449795 81630 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165545 81630 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 432 3 0 4 4.1 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm5003952
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm5003952
58258871 127432 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cnc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664779 127432 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 2 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cnc5[nH]ccc5c4)ccc31)C1CCC(C2)N1 nan
58258857 128460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
53320775 59813 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642878 59813 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739546 59813 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 2.8 CN(C)CCNC(=O)c1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
53259021 69404 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935594 69404 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 359 2 1 4 3.8 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2011.11.050
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070521y
45484399 197286 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585098 197286 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 NCCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836824 18524 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277467 18524 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 4 1 6 2.3 CCn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44554227 18563 0 None 33 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277837 18563 0 None 33 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 1 6 4.0 CC(C)n1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
57398803 69399 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
CHEMBL1935589 69399 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
CHEMBL1949758 69399 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.12.026
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/acs.jmedchem.5b00179
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HeLa cells after 60 mins by scintillation spectrometry
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/acs.jmedchem.5b00179
68115703 131236 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc(C(C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692977 131236 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc(C(C)O)cc2)cc2c3c(oc12)CCNC3 nan
25024727 62641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/ml100101u
CHEMBL1785074 62641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1021/ml100101u
11176859 62975 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm5003952
CHEMBL179344 62975 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3cccc4ccccc34)cc21 10.1021/jm5003952
10091667 113662 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 6 1 4 3.6 O=S(=O)(c1cccc(F)c1)c1c[nH]c2c(OCCN3CCCC3)cccc12 10.1021/jm5003952
CHEMBL3329431 113662 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 388 6 1 4 3.6 O=S(=O)(c1cccc(F)c1)c1c[nH]c2c(OCCN3CCCC3)cccc12 10.1021/jm5003952
58258863 127444 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc5occc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664791 127444 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 5 4.1 Cn1c2c(c3cc(S(=O)(=O)c4ccc5occc5c4)ccc31)C1CCC(C2)N1 nan
6918515 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
71 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1016/j.bmcl.2005.01.031
44388955 62756 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178869 62756 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1ccccc1)n1cc(C2CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44389086 123232 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL362220 123232 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
12147013 65251 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL183203 65251 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
11747350 106848 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 106848 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
6918515 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
71 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1007/s00044-004-0121-8
3950432 168942 8 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 373 5 0 5 4.1 CC(CSc1nc2ccccc2c(=O)n1-c1ccc(Cl)cc1)N(C)C 10.1016/j.ejmech.2019.111857
CHEMBL4434670 168942 8 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 373 5 0 5 4.1 CC(CSc1nc2ccccc2c(=O)n1-c1ccc(Cl)cc1)N(C)C 10.1016/j.ejmech.2019.111857
6918515 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
71 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm030030n
11747350 106848 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm030030n
CHEMBL317535 106848 0 None 2 10 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm030030n
10713238 206091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 355 4 3 4 2.9 CNc1cc(Br)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
CHEMBL96317 206091 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 355 4 3 4 2.9 CNc1cc(Br)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
6918515 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
44438732 93459 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 0 2 4.4 CN(C)CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL248085 93459 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 0 2 4.4 CN(C)CCc1cn(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
137644521 157931 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 391 3 1 5 4.1 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1cccc2ccccc12 10.1021/acsmedchemlett.6b00482
CHEMBL4090862 157931 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 391 3 1 5 4.1 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1cccc2ccccc12 10.1021/acsmedchemlett.6b00482
66801537 157389 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4084492 157389 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155515942 169442 0 None 70 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4442456 169442 0 None 70 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2ncccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
155517413 169609 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
CHEMBL4444655 169609 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 403 3 1 5 4.1 Cc1c(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
2865 4079 67 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
59 4079 67 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
60854 4079 67 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
CHEMBL708 4079 67 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
DB00246 4079 67 None -83 53 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.ejmech.2018.01.002
121238068 156668 0 None 281 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4076046 156668 0 None 281 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 334 3 1 6 2.0 CN1CCN(c2nc(N)nc(Cc3cccc4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
118654345 190315 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5185190 190315 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 469 4 1 5 4.0 O=S(=O)(c1ccccc1Br)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
126720425 161565 0 None 34 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161308 161565 0 None 34 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 4 1 5 3.7 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137640158 156233 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 6 0 6 3.2 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4070785 156233 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 6 0 6 3.2 CCN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
44403083 132985 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1cccc(Cl)c1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370719 132985 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1cccc(Cl)c1Cl)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403077 140274 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 424 4 1 5 4.0 O=S(=O)(c1ccc(Br)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL381887 140274 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 424 4 1 5 4.0 O=S(=O)(c1ccc(Br)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
16718869 181911 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 486 6 1 4 6.5 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2C1 10.1021/jm8009469
CHEMBL478686 181911 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 486 6 1 4 6.5 CC1=C(CCN2CCCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2C1 10.1021/jm8009469
12147013 65251 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL183203 65251 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 328 5 0 4 3.0 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
151199471 172270 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2cc(N3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4514440 172270 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1CCc2cc(N3CCNCC3)ccc21 10.1016/j.bmcl.2016.07.055
71151924 117739 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(F)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409240 117739 0 None -3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(F)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
6918515 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
71 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometryDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/acs.jmedchem.5b00179
68115645 131187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 2 1 5 3.6 O=S(=O)(c1cncc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692928 131187 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 382 2 1 5 3.6 O=S(=O)(c1cncc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115677 131203 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692944 131203 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23652993 56400 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 481 4 0 5 4.4 CCN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642425 56400 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 481 4 0 5 4.4 CCN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
16222548 81645 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165560 81645 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
58158668 138499 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785864 138499 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 3 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
53327973 111166 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286399 111166 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
44386851 130044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 6 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL368132 130044 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 6 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)Cc2ccccc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
10777767 203362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 0 3 3.2 CCCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL7732 203362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 260 6 0 3 3.2 CCCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
10757046 106757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 306 5 4 5 2.2 CNc1cc(NC)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
CHEMBL316855 106757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 306 5 4 5 2.2 CNc1cc(NC)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm030030n
66801561 155536 0 None -660 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4062817 155536 0 None -660 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 477 8 2 3 5.3 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
66801295 156599 0 None -117 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4075144 156599 0 None -117 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
71451459 81032 0 None -33 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159487 81032 0 None -33 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
10480841 157639 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 492 5 0 7 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc([N+](=O)[O-])cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4087748 157639 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 492 5 0 7 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc([N+](=O)[O-])cc23)CC1 10.1021/acs.jmedchem.6b01662
22028187 195981 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL570971 195981 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
145946527 167009 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4217761 167009 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL4300609 167009 0 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 382 10 0 4 3.6 Cc1cccc(OCCOCCN2CCN(CCc3ccccc3)CC2)c1C 10.1016/j.bmcl.2018.04.059
CHEMBL5071978 212501 0 None -29 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
2389 3279 114 None -2454 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 3279 114 None -2454 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 3279 114 None -2454 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 3279 114 None -2454 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 3279 114 None -2454 67 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
145966418 163689 0 None -36 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3cccc(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4211253 163689 0 None -36 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3cccc(Cl)c3)CC1)C2 10.1016/j.bmcl.2018.06.019
13069624 120090 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360991 120090 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3545931 120090 0 None -34 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 382 5 0 8 0.6 Cn1c(=O)c2c(ncn2CCCN2CCN(c3ccccc3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
155539573 172300 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 2 2 5.9 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)o3)cccc2c1 10.1016/j.ejmech.2019.111857
CHEMBL4515249 172300 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 2 2 5.9 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)o3)cccc2c1 10.1016/j.ejmech.2019.111857
144950987 179390 0 None -165 6 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4746800 179390 0 None -165 6 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 292 3 0 2 3.4 CN(C)CCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
71451460 81033 0 None -50 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159488 81033 0 None -50 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
162649787 179396 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1cc(N2CCN(CC(F)(F)F)CC2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4746839 179396 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1cc(N2CCN(CC(F)(F)F)CC2)c2ccccc21 10.1016/j.ejmech.2020.112916
13069603 120096 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360993 120096 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546107 120096 0 None -112 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 416 5 0 8 1.3 Cn1c(=O)c2c(ncn2CCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57402072 71128 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949770 71128 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962398 71128 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 7 1 6 2.8 COCCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
57401516 68057 0 None -63 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 7 1 5 3.0 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL1916746 68057 0 None -63 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 7 1 5 3.0 CN1C(=O)N(CC(O)CN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
155552799 175731 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4545270 175731 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595236 175731 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
44413645 79744 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1ccc2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
CHEMBL213407 79744 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 355 3 2 5 3.4 CNc1ccc2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
59339309 138599 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 351 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1ccc(N(C)C)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3786951 138599 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 351 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1ccc(N(C)C)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
118626042 165018 0 None -257 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242170 165018 0 None -257 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
57402070 71219 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71219 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71219 0 None -5 2 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
155547693 172999 0 None 3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
CHEMBL4532712 172999 0 None 3 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1cccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2019.06.022
164619282 185221 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 387 8 2 4 3.9 Cc1cccc(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4866962 185221 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 387 8 2 4 3.9 Cc1cccc(CNCCOc2cccc3c2[nH]c(=O)n3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
118724648 115965 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361005 115965 0 None -9 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 515 7 0 10 1.5 Cn1c(=O)c2c(nc(N3CCOCC3)n2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
49836721 18512 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 3 2 5 2.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277375 18512 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 3 2 5 2.8 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
25263337 184113 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL485016 184113 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 330 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1O[C@H](C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
164620748 185663 0 None 5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873623 185663 0 None 5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
58258766 128461 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 417 3 1 6 3.4 COc1cc(S(=O)(=O)c2cncc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669660 128461 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 417 3 1 6 3.4 COc1cc(S(=O)(=O)c2cncc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44390045 12668 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
CHEMBL1187981 12668 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
CHEMBL534698 12668 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 240 2 1 2 2.8 CCc1cc(N2CCNCC2)c2ccccc2c1 10.1016/j.bmcl.2005.01.031
155540673 171966 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 367 2 3 3 2.5 N=C(NC1=NC2CCCCC2C(=O)N1)N1CCC(Cc2ccccc2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4483706 171966 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 367 2 3 3 2.5 N=C(NC1=NC2CCCCC2C(=O)N1)N1CCC(Cc2ccccc2)CC1 10.1016/j.ejmech.2019.111857
11849194 79408 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212063 79408 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
155548677 173156 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.8 COc1ccc2[nH]c(C)c(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4536315 173156 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.8 COc1ccc2[nH]c(C)c(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
126720417 161549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4161125 161549 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
164610456 183918 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4847379 183918 0 None 4 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
53327973 111166 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286399 111166 0 None 22 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
46880533 6095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 1 4 4.6 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081120 6095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 1 4 4.6 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
11849194 79408 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL212063 79408 1 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
44405385 140087 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL381415 140087 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2005.08.059
155523121 170273 0 None 58 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 7 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(NCC(F)F)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4453733 170273 0 None 58 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 446 7 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(NCC(F)F)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155542237 172520 0 None 56 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 472 7 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4520003 172520 0 None 56 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 472 7 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
23655290 148547 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 318 4 1 4 2.5 NCCc1cn(S(=O)(=O)c2ccc(F)cc2)c2ccccc12 10.1021/jm070521y
CHEMBL394302 148547 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 318 4 1 4 2.5 NCCc1cn(S(=O)(=O)c2ccc(F)cc2)c2ccccc12 10.1021/jm070521y
155551102 173386 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4541473 173386 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
57391618 71125 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71125 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71125 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57391569 71181 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949929 71181 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962864 71181 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
68109184 131111 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2ccccc2c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692853 131111 0 None - 1 Human 7.7 pKi = 7.7 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2ccccc2c1)c1ccc2oc3c(c2c1)CNCC3 nan
25117679 198920 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599263 198920 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
10295665 130858 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 4 4.3 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5cccnc45)cc23)CC1 10.1021/jm049615n
CHEMBL368959 130858 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 4 4.3 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5cccnc45)cc23)CC1 10.1021/jm049615n
44403063 71411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccccc1C(F)(F)F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196661 71411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1ccccc1C(F)(F)F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
162665588 181814 0 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
CHEMBL4785434 181814 0 None -48 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
56593642 65348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834334 65348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
44413493 138050 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 386 4 1 6 3.4 COc1cc(OC)c2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
CHEMBL377546 138050 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 386 4 1 6 3.4 COc1cc(OC)c2c3c(n(S(=O)(=O)c4ccc(N)cc4)c2c1)CCCC3 10.1016/j.bmcl.2006.04.094
44438718 93420 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 5 0 4 3.3 CN(C)CCc1cn(S(=O)(=O)C2CCCCC2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247872 93420 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 334 5 0 4 3.3 CN(C)CCc1cn(S(=O)(=O)C2CCCCC2)c2ccccc12 10.1016/j.bmcl.2006.12.089
56944864 157018 0 None -83 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 8 2 3 5.0 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4080369 157018 0 None -83 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 457 8 2 3 5.0 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
155557143 173978 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 414 7 2 3 6.1 COc1ccc2[nH]cc(CCNCc3ccc(-c4cc(Cl)cc(Cl)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4556193 173978 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 414 7 2 3 6.1 COc1ccc2[nH]cc(CCNCc3ccc(-c4cc(Cl)cc(Cl)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
56944764 111604 0 None -190 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289990 111604 0 None -190 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 417 6 1 5 3.4 Cc1cccc(S(=O)(=O)NCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1021/jm401895u
127032187 138547 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(OC)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786432 138547 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(OC)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
162647241 178905 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2020.112916
CHEMBL4740955 178905 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2020.112916
127046634 139452 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 449 5 2 4 3.8 COc1cccc(C(C(=O)NC(C)(C)C)N2CCc3c([nH]c4ccccc34)CC2=O)c1OC 10.1016/j.bmcl.2016.03.036
CHEMBL3799903 139452 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 449 5 2 4 3.8 COc1cccc(C(C(=O)NC(C)(C)C)N2CCc3c([nH]c4ccccc34)CC2=O)c1OC 10.1016/j.bmcl.2016.03.036
162675372 182713 0 None -2 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 361 4 0 3 3.5 CN1CCN(CCCN2C(=O)c3ccccc3/C=C\c3ccccc32)CC1 10.1016/j.bmcl.2020.127493
CHEMBL4796968 182713 0 None -2 4 Human 4.7 pKi = 4.7 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 361 4 0 3 3.5 CN1CCN(CCCN2C(=O)c3ccccc3/C=C\c3ccccc32)CC1 10.1016/j.bmcl.2020.127493
71458648 81003 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 4 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159459 81003 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 4 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
90666899 108957 0 None -42 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
CHEMBL3220215 108957 0 None -42 7 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
4543 169982 36 None -9 29 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm2011657
CHEMBL1201156 169982 36 None -9 29 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm2011657
CHEMBL445 169982 36 None -9 29 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 10.1021/jm2011657
45487112 197183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2nc(Cl)ccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583896 197183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 363 5 0 5 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2nc(Cl)ccc21 10.1016/j.bmcl.2009.10.067
168272182 189812 0 None -4 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5177716 189812 0 None -4 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 433 5 0 6 3.5 O=c1n(Cc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2)nc2ccccn12 10.1016/j.ejmech.2022.114319
49781034 17000 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.0 COc1ccc(N(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256254 17000 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.0 COc1ccc(N(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
145946265 166953 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4203310 166953 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4299892 166953 0 None -3 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
57399091 68081 0 None -57 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2011.09.044
CHEMBL1917344 68081 0 None -57 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2cccc3cccnc23)CC1 10.1016/j.bmc.2011.09.044
16718826 174834 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 494 7 1 3 6.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2/C1=C\c1ccccc1 10.1021/jm8009469
CHEMBL457569 174834 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 494 7 1 3 6.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2/C1=C\c1ccccc1 10.1021/jm8009469
156009483 176492 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 412 5 1 5 2.8 C#CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4632872 176492 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 412 5 1 5 2.8 C#CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
57393365 71206 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
162676728 183001 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 4.2 O=S(=O)(C1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4800552 183001 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 4.2 O=S(=O)(C1CCCCC1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
155542267 172525 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 475 7 0 6 5.3 CCCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
CHEMBL4520176 172525 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 475 7 0 6 5.3 CCCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
162663493 181420 0 None -41 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4780536 181420 0 None -41 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 572 10 3 7 3.9 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(N)c(Br)c2)CC1 10.1016/j.ejmech.2016.05.048
162676234 182747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(N2CCCCC2)c2ccccc21 10.1016/j.ejmech.2020.112916
CHEMBL4797400 182747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1cc(N2CCCCC2)c2ccccc21 10.1016/j.ejmech.2020.112916
25263318 190890 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 2 5.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL519359 190890 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 4 1 2 5.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
58258847 127420 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(Cl)c31)C1CCC(C2)N1 nan
CHEMBL3664766 127420 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(Cl)c31)C1CCC(C2)N1 nan
58258850 127442 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cnccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664789 127442 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cnccc45)ccc31)C1CCC(C2)N1 nan
155551834 173453 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4543169 173453 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
137642224 157546 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4086515 157546 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2017.04.033
137642224 157546 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2022.114645
CHEMBL4086515 157546 0 None 81 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 323 3 2 6 1.3 CN1CCN(c2nc(N)nc(Cc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2022.114645
44403075 71457 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196791 71457 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 372 3 1 4 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403053 165411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1cccc(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL425197 165411 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1cccc(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398717 69401 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935591 69401 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
164612743 184124 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 451 9 1 7 4.0 O=[N+]([O-])c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4850275 184124 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 451 9 1 7 4.0 O=[N+]([O-])c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
137210067 139555 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 428 5 1 7 3.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(O)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800539 139555 0 None 4 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 428 5 1 7 3.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(O)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
22028185 197362 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL585931 197362 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836925 18513 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
CHEMBL1277376 18513 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(N3CCNCC3)ccc12 10.1021/jm1007825
24784325 175613 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 385 4 1 6 3.2 CC(C)c1ccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)cc1 10.1016/j.bmcl.2008.12.107
CHEMBL459347 175613 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 385 4 1 6 3.2 CC(C)c1ccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)cc1 10.1016/j.bmcl.2008.12.107
24784573 175614 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459348 175614 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
118731502 117731 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 505 9 1 4 6.5 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409232 117731 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 505 9 1 4 6.5 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(Cc5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
66801107 111554 0 None -16 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289709 111554 0 None -16 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 430 7 1 6 3.1 Cc1cccc(S(=O)(=O)NCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
11429601 200092 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606763 200092 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
44155871 60661 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762571 60661 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
57400392 69410 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935600 69410 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 387 2 1 5 3.2 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCOC1)NCC3 10.1016/j.bmcl.2011.11.050
44403090 123463 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL362921 123463 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44438711 93500 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 322 8 0 4 3.1 CCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL248268 93500 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 322 8 0 4 3.1 CCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
66801344 158875 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4100951 158875 0 None -58 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155523771 170342 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 6 2 4 4.5 c1ccc2c(CCNCc3ccc(-c4ccc5c(c4)OCO5)o3)c[nH]c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4454873 170342 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 6 2 4 4.5 c1ccc2c(CCNCc3ccc(-c4ccc5c(c4)OCO5)o3)c[nH]c2c1 10.1016/j.ejmech.2019.111857
71574204 85840 0 None -27 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312640 85840 0 None -27 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
24777063 155038 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@@H]1CCCN1C 10.1021/jm070910s
CHEMBL404421 155038 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 272 4 1 2 3.4 CCc1[nH]c2ccc(OC)cc2c1C[C@@H]1CCCN1C 10.1021/jm070910s
145963830 163571 0 None -21 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 163571 0 None -21 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
90644075 111587 0 None -34 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 8 1 7 3.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289973 111587 0 None -34 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 8 1 7 3.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
10331436 321 7 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 321 7 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 321 7 None -1096 6 Human 5.7 pKi = 5.7 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
156012741 176713 0 None -100 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.4 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4636435 176713 0 None -100 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.4 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2020.115459
57396857 71224 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949971 71224 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963101 71224 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 472 9 1 5 4.2 O=S(=O)(NCCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
145983794 165102 0 None -18 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cncc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4244280 165102 0 None -18 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cncc2ccccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
156019370 177383 0 None -54 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 9 1 5 4.4 O=C(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
CHEMBL4645793 177383 0 None -54 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 9 1 5 4.4 O=C(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
155519599 175739 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4447594 175739 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595274 175739 0 None -40 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.2 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
134146185 148305 0 None -50 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2cccnc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3941102 148305 0 None -50 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 512 10 1 5 4.6 O=C(CCOCCN1CCN(c2cccnc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
24966737 83615 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 4 0 5 3.6 Cc1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207380 83615 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 4 0 5 3.6 Cc1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44155871 60661 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762571 60661 0 None - 1 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 347 5 1 7 1.6 Cc1cc(C)n2nc(OCCO)c(S(=O)(=O)c3ccccc3)c2n1 nan
162655077 180015 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 580 12 1 5 6.9 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4754407 180015 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 580 12 1 5 6.9 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
2389 3279 114 None -2454 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
5073 3279 114 None -2454 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
96 3279 114 None -2454 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
CHEMBL85 3279 114 None -2454 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
DB00734 3279 114 None -2454 67 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2010.07.105
11283016 60161 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 7 2 7 3.4 CCN(CC)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
CHEMBL175488 60161 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 7 2 7 3.4 CCN(CC)C(=O)C(=O)c1c[nH]c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc12 10.1021/jm049615n
168275185 190062 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 389 3 0 4 4.7 Clc1cccc(Cn2ccc3c(N4CC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5181534 190062 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 389 3 0 4 4.7 Clc1cccc(Cn2ccc3c(N4CC5(COC5)C4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
71453279 81020 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cc(Cl)ccc2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159475 81020 0 None -3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cc(Cl)ccc2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
155545088 176083 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4528793 176083 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598089 176083 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
58258760 127447 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 6 3.3 Cn1c2c(c3cc(S(=O)(=O)c4ccc5c(ccn5CCO)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664794 127447 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 435 4 2 6 3.3 Cn1c2c(c3cc(S(=O)(=O)c4ccc5c(ccn5CCO)c4)ccc31)C1CCC(C2)N1 nan
57334553 90044 0 None -758 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1016/j.bmcl.2021.127909
CHEMBL2387229 90044 0 None -758 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 484 7 0 6 6.1 Cc1cc(=O)oc2c(Cl)c(OCCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1016/j.bmcl.2021.127909
142601337 185388 0 None -72 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4869695 185388 0 None -72 5 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
58258806 127443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
44395570 65927 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c2c1 10.1016/j.bmcl.2004.09.003
CHEMBL184640 65927 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1ccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c2c1 10.1016/j.bmcl.2004.09.003
44341344 9383 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 6 1 5 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL111943 9383 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 6 1 5 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
44567981 188812 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1ccc(F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL513051 188812 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1ccc(F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
145984065 165198 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246630 165198 0 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
155519102 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4447416 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
126720428 181666 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 415 5 1 8 2.2 COc1cccc(S(=O)(=O)n2c(C(C)C)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4783584 181666 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 415 5 1 8 2.2 COc1cccc(S(=O)(=O)n2c(C(C)C)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
46933237 62206 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782360 62206 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
44403073 69981 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 6 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL194465 69981 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 6 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
155519102 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4447416 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164624246 185361 0 None 5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4869411 185361 0 None 5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155522920 170236 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4453250 170236 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 474 5 2 6 4.7 COc1ccc2c(c1)c(-c1[nH]c(NC(C)=O)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
11709684 196940 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
CHEMBL578826 196940 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmcl.2009.10.067
11709684 196940 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL578826 196940 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
155552380 173491 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4544099 173491 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 370 4 0 3 3.6 CCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
71151591 117749 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2F)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409250 117749 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2F)CC1 10.1016/j.ejmech.2014.12.045
57398615 71205 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71205 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71205 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
56944287 111612 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 9 1 6 4.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289998 111612 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 515 9 1 6 4.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
66801565 111635 0 None -17 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3290020 111635 0 None -17 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 474 7 1 7 4.1 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
53325160 56396 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 475 4 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642421 56396 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 475 4 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2010.11.001
46880756 5950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080380 5950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 4.2 O=S(=O)(c1cccc2ccccc12)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
24965330 83609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207374 83609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2012.10.057
68638941 157200 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4082319 157200 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
56595529 65314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
CHEMBL1834234 65314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1016/j.bmcl.2016.02.001
56595529 65314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
CHEMBL1834234 65314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccccc1 10.1021/jm200466r
53327974 111198 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286582 111198 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
53328000 111208 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286591 111208 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
11849197 138336 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.4 NCCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378179 138336 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.4 NCCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
23815446 110093 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 443 9 1 6 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL325428 110093 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 443 9 1 6 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
1355 1980 82 None -125 15 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 1980 82 None -125 15 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 1980 82 None -125 15 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 1980 82 None -125 15 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
66801267 111593 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289979 111593 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 484 7 1 6 4.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
136118619 75898 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 75898 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
127045665 139535 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 429 5 1 7 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(=O)[nH]c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800442 139535 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 429 5 1 7 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(=O)[nH]c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
56595408 65313 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
CHEMBL1834232 65313 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC(C)=N1 10.1021/jm200466r
145982506 164843 0 None -162 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238029 164843 0 None -162 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
162676054 182663 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 587 14 2 6 5.7 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4796358 182663 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 587 14 2 6 5.7 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
164625434 184926 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 8 1 3 4.9 c1ccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4862516 184926 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 356 8 1 3 4.9 c1ccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
127038033 136083 0 None -33 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 453 8 1 5 4.2 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3ncccc23)CC1 10.1039/C5MD00166H
CHEMBL3739680 136083 0 None -33 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 453 8 1 5 4.2 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3ncccc23)CC1 10.1039/C5MD00166H
162655547 180214 0 None -54 5 Human 4.6 pKi = 4.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4756446 180214 0 None -54 5 Human 4.6 pKi = 4.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 306 4 0 2 3.8 CN(C)CCCN1C(=O)c2ccccc2/C=C\c2ccccc21 10.1016/j.bmcl.2020.127493
155566439 175225 0 None 12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2019.06.022
CHEMBL4584325 175225 0 None 12 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccc(OCc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2019.06.022
57403837 71129 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71129 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71129 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
155520553 175935 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4449590 175935 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596888 175935 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 6.0 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
1472656 34405 22 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1429795 34405 22 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
1472656 34405 22 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1429795 34405 22 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 287 2 0 5 2.2 Cc1cc(C)n2ncc(S(=O)(=O)c3ccccc3)c2n1 nan
137633855 156082 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(F)cc3)c2c1 10.1021/acs.jmedchem.6b01662
CHEMBL4069113 156082 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(F)cc3)c2c1 10.1021/acs.jmedchem.6b01662
25263333 178895 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.7 Cc1c(C2CCNCC2)ccnc1OCc1ccc(F)cc1F 10.1016/j.bmcl.2009.03.077
CHEMBL474088 178895 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.7 Cc1c(C2CCNCC2)ccnc1OCc1ccc(F)cc1F 10.1016/j.bmcl.2009.03.077
58258831 128445 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 431 2 1 5 4.2 Cn1c2c(c3cc(S(=O)(=O)n4c5c(c6ccccc64)CCC5)ccc31)C1CCC(C2)N1 nan
CHEMBL3669644 128445 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 431 2 1 5 4.2 Cn1c2c(c3cc(S(=O)(=O)n4c5c(c6ccccc64)CCC5)ccc31)C1CCC(C2)N1 nan
1212 1632 45 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -48 65 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
53318142 59774 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642867 59774 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739135 59774 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
53322082 59843 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642875 59843 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739701 59843 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 462 6 2 5 4.4 O=C(CCN1CCCCC1)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44568021 191987 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 410 2 1 4 4.4 O=S(=O)(c1ccc2c(Cl)cccc2c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL521426 191987 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 410 2 1 4 4.4 O=S(=O)(c1ccc2c(Cl)cccc2c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
155518290 169692 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4446018 169692 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
53327974 111198 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286582 111198 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
53328000 111208 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
CHEMBL3286591 111208 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1cccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)c1 10.1021/jm5003759
164626757 185712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 514 9 1 7 5.1 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4874372 185712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 514 9 1 7 5.1 CC(=O)Oc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.ejmech.2021.113792
127047900 139390 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3C(F)(F)F)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799547 139390 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccccc3C(F)(F)F)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
71151664 117748 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 468 9 1 5 4.4 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409249 117748 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 468 9 1 5 4.4 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
11476019 200612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 6 2 4 4.3 COc1ccc(Cl)cc1S(=O)(=O)Nc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm049243i
CHEMBL610258 200612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 6 2 4 4.3 COc1ccc(Cl)cc1S(=O)(=O)Nc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm049243i
68115813 131748 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 297 2 1 2 4.3 Clc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696983 131748 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 297 2 1 2 4.3 Clc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
25056080 65359 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834345 65359 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1016/j.bmcl.2016.02.001
25056080 65359 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
CHEMBL1834345 65359 0 None 407 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 3 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)(C)C=N1 10.1021/jm200466r
56595405 65309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
70878688 65309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
CHEMBL1834229 65309 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCC1C=NN(/C(N)=N/S(=O)(=O)c2cccc(Cl)c2)C1 10.1021/jm200466r
16223066 81620 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165536 81620 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
10158456 129570 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 409 4 2 4 4.5 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(Cl)s4)cc23)CC1 10.1021/jm049615n
CHEMBL367730 129570 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 409 4 2 4 4.5 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(Cl)s4)cc23)CC1 10.1021/jm049615n
25117677 198568 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL597009 198568 0 None 23 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 4 1 5 3.7 CN(C)[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
162650396 179505 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4748107 179505 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
25263348 183788 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccc(Cl)cc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484532 183788 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccc(Cl)cc2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
16222962 81621 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.2 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165537 81621 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.2 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(F)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
10800458 202652 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 0 3 2.8 CCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL7166 202652 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 0 3 2.8 CCn1cc(CCN(C)C)c2cc(OC)ccc21 10.1021/jm990550b
CHEMBL5094680 213734 0 None -15 8 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
71454999 81010 0 None -794 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159465 81010 0 None -794 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
127040442 136344 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccccc2F)CC1 10.1039/C5MD00166H
CHEMBL3742076 136344 0 None -4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2ccccc2F)CC1 10.1039/C5MD00166H
155554556 173825 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 452 9 0 4 5.3 CN(CCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2019.07.040
CHEMBL4552323 173825 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cells measured after 60 mins by microbeta scintillation counting method
ChEMBL 452 9 0 4 5.3 CN(CCCN1CCN(c2cccc3c2ccn3Cc2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2019.07.040
90656171 110353 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 4 1 4 4.2 O=C1OC(c2ccccc2Cl)CN1c1cccc(OC2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260804 110353 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 4 1 4 4.2 O=C1OC(c2ccccc2Cl)CN1c1cccc(OC2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
44396965 12670 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL1187985 12670 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL534703 12670 2 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
2950739 162413 10 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4174845 162413 10 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 4 4.6 COc1ccc(CNCCC(c2ccco2)c2ccccc2OC)cc1 10.1016/j.ejmech.2018.04.010
129103161 166517 0 None -51 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4289498 166517 0 None -51 13 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
10478367 71326 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196370 71326 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL430500 71326 0 None -478 7 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
137652044 156625 0 None -13 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4075422 156625 0 None -13 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
155561581 175067 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 6 -0.3 CN1CCN(c2nc(N)nc(C[Se]c3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4580959 175067 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 364 4 1 6 -0.3 CN1CCN(c2nc(N)nc(C[Se]c3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
145947937 167162 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4207653 167162 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4302655 167162 0 None -478 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]LSD from recombinant human 5-HT6 receptor expressed in CHO cells cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
57403833 71126 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71126 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71126 0 None -6 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
58258825 128442 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 2 5 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5cc[nH]n5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669641 128442 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 2 5 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5cc[nH]n5)c4)ccc31)C1CCC(C2)N1 nan
155543250 172727 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 275 1 1 2 3.3 Cn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4526012 172727 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 275 1 1 2 3.3 Cn1cncc1-c1c[nH]c2ccc(Br)cc12 10.1016/j.ejmech.2019.03.017
71453281 81030 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159485 81030 0 None -61 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 422 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.ejmech.2012.07.043
90468605 184460 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 266 1 1 3 2.5 CN1CCN(c2nc3ccccc3c3[nH]ccc23)CC1 10.1021/acs.jmedchem.1c00224
CHEMBL4855303 184460 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 266 1 1 3 2.5 CN1CCN(c2nc3ccccc3c3[nH]ccc23)CC1 10.1021/acs.jmedchem.1c00224
2855326 93608 13 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccc(OCCNc2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])cc1 10.1016/j.bmcl.2007.09.016
CHEMBL248845 93608 13 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 386 8 1 7 2.8 COc1ccc(OCCNc2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])cc1 10.1016/j.bmcl.2007.09.016
8447 188362 80 None -33 13 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -33 13 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
138691321 173947 0 None -67 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2c(F)cc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4555349 173947 0 None -67 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2c(F)cc(I)cc12 10.1016/j.ejmech.2019.03.017
44388971 122254 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 428 5 0 4 5.2 O=S(=O)(c1ccccc1)n1cc(C2=CCN(Cc3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL360475 122254 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 428 5 0 4 5.2 O=S(=O)(c1ccccc1)n1cc(C2=CCN(Cc3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
155538451 171821 0 None -9 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 485 10 0 5 5.2 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4476432 171821 0 None -9 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 485 10 0 5 5.2 CCOc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
11430512 167716 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 3 0 4 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL433979 167716 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 436 3 0 4 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4ccccc34)CC1)C(=O)OC2 10.1021/jm049615n
155533990 171309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 461 6 0 6 4.9 CCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
CHEMBL4469325 171309 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 461 6 0 6 4.9 CCCN1CC=C(c2cn(S(=O)(=O)c3ccc4cccnc4c3)c3ccc(OC)cc23)CC1 10.1021/acsmedchemlett.6b00056
155568249 175535 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4cccc(OC)c34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4591630 175535 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4cccc(OC)c34)o2)c1 10.1016/j.ejmech.2019.111857
71456782 81024 0 None -27 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 364 7 1 4 2.3 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159479 81024 0 None -27 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 364 7 1 4 2.3 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
67268994 163416 2 None -7 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4207884 163416 2 None -7 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 247 1 2 2 2.4 Clc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
57396419 71198 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1949976 71198 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
CHEMBL1962961 71198 0 None -616 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cnc2ccccc2c1)N1CCC(CCN2CCN(c3ccc(Cl)cc3)CC2)CC1 10.1016/j.bmc.2011.12.039
44395664 66427 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
CHEMBL185850 66427 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 358 6 0 5 3.0 COc1cccc2c(S(=O)(=O)c3ccccc3)cn(CCN(C)C)c12 10.1016/j.bmcl.2004.09.003
10017687 66945 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL188182 66945 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.09.003
9905247 106765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm010943m
CHEMBL316881 106765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm010943m
155516118 169472 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 3 4 4.0 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4442855 169472 2 None 1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 3 4 4.0 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
44240802 138651 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787508 138651 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 375 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)CCN2)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
2771419 154203 24 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 5 2 6 2.2 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccco1 10.1016/j.bmcl.2007.09.016
CHEMBL399962 154203 24 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 5 2 6 2.2 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccco1 10.1016/j.bmcl.2007.09.016
44403074 69945 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 4 1 5 3.9 O=S(=O)(c1ccc(Cl)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194311 69945 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 4 1 5 3.9 O=S(=O)(c1ccc(Cl)s1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
155518159 169709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4446215 169709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 394 4 2 5 3.5 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
10017687 66945 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
CHEMBL188182 66945 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 300 4 1 4 2.4 NCCn1cc(S(=O)(=O)c2ccccc2)c2ccccc21 10.1016/j.bmc.2009.05.055
24784575 176140 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
CHEMBL459989 176140 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 373 4 1 7 2.1 COc1cccc(S(=O)(=O)c2cccc3oc(N4CCNCC4)nc23)c1 10.1016/j.bmcl.2008.12.107
155565138 174971 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4578632 174971 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
155566852 175309 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4586276 175309 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
56943695 111630 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290015 111630 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 505 7 1 6 5.2 Cc1c(S(=O)(=O)NCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68108636 131152 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
CHEMBL3692893 131152 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.0 CC1Cc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2CN1 nan
68115684 131210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692951 131210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 3 2 5 3.8 CC(C)(O)c1ccccc1S(=O)(=O)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
10069527 158383 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4095670 158383 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
17940185 119083 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C(F)(F)F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL346227 119083 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.6 COc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C(F)(F)F)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
6918576 205981 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 436 4 2 5 3.8 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(01)00558-3
CHEMBL95628 205981 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 436 4 2 5 3.8 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(01)00558-3
9905247 106765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm050247c
CHEMBL316881 106765 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 322 5 0 4 3.4 COc1ccc2c(c1)c(CCN(C)C)cn2C(=O)c1ccccc1 10.1021/jm050247c
134132432 144207 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3908917 144207 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
46889857 7013 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 5 1 5 3.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCCC2CNc1ncccn1 10.1016/j.bmcl.2010.03.110
CHEMBL1085112 7013 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 5 1 5 3.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)CCCC2CNc1ncccn1 10.1016/j.bmcl.2010.03.110
17978385 71360 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1ccc2ccccc2c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196524 71360 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1ccc2ccccc2c1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
10149997 127004 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)nccc12 10.1016/j.bmcl.2005.06.107
CHEMBL366248 127004 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)nccc12 10.1016/j.bmcl.2005.06.107
44425703 86240 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 417 4 1 4 4.1 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(C#N)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231640 86240 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 417 4 1 4 4.1 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(C#N)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
11163741 141573 5 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNCC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL388247 141573 5 None -2 5 Human 7.6 pKi = 7.6 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 2 3 3.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNCC3)cc1 10.1016/j.bmcl.2006.10.036
53323873 56405 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 453 4 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642430 56405 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 453 4 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
53327999 111207 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286590 111207 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
66801425 156644 0 None -83 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4075673 156644 0 None -83 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 441 8 2 3 4.5 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
66801837 156986 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 507 8 2 3 6.1 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4079972 156986 0 None -2 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 507 8 2 3 6.1 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
137654666 158070 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4092243 158070 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 463 7 2 3 4.9 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
2845118 153549 10 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 3 0 6 2.1 Cc1cc(C)n(-c2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
CHEMBL398482 153549 10 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 3 0 6 2.1 Cc1cc(C)n(-c2cc(N3CCN(C)CC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
155515416 176030 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4442148 176030 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4597708 176030 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 4 1 5 3.3 COc1ccc2c(c1)c(-c1[nH]c3nccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
56944859 111616 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290001 111616 0 None -354 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 453 6 1 5 4.3 O=S(=O)(NCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
2928642 161739 9 None 3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 7 1 2 6.1 Cc1ccc(C(CCNC(C)c2ccc(Cl)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4164143 161739 9 None 3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 353 7 1 2 6.1 Cc1ccc(C(CCNC(C)c2ccc(Cl)cc2)c2ccco2)cc1 10.1016/j.ejmech.2018.04.010
90654844 112127 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233671 112127 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302598 112127 0 None -33 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 466 9 0 4 4.4 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.ejmech.2014.01.065
44398569 68816 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 458 9 1 5 3.9 CC[N+](C)(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1021/jm050247c
CHEMBL192435 68816 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 458 9 1 5 3.9 CC[N+](C)(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccc(OC)cc12 10.1021/jm050247c
127031619 138503 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 406 4 2 4 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(O)cc1 10.1016/j.bmcl.2016.02.001
CHEMBL3785894 138503 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 406 4 2 4 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccc(O)cc1 10.1016/j.bmcl.2016.02.001
6623 162770 93 None - 1 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL418971 162770 93 None - 1 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 228 2 2 2 3.4 CC(C)(c1ccc(O)cc1)c1ccc(O)cc1 nan
76284193 146064 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 444 10 1 5 3.6 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1016/j.ejmech.2016.05.005
CHEMBL3923145 146064 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 444 10 1 5 3.6 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccncc1 10.1016/j.ejmech.2016.05.005
156021059 177563 0 None -50 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 8 3.5 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)nc2ccccn12 10.1016/j.bmc.2020.115459
CHEMBL4648581 177563 0 None -50 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 436 8 0 8 3.5 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)nc2ccccn12 10.1016/j.bmc.2020.115459
68108826 131158 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 418 3 1 5 3.2 CN(C)C(=O)C1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692899 131158 0 None - 1 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 418 3 1 5 3.2 CN(C)C(=O)C1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
44403079 134704 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 312 2 1 4 2.5 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
CHEMBL372373 134704 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 312 2 1 4 2.5 O=S(=O)(c1ccccc1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
44568104 183473 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482260 183473 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.6 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
4301799 124285 11 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 222 2 2 1 3.3 Nc1ccc(Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL364248 124285 11 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 222 2 2 1 3.3 Nc1ccc(Cc2c[nH]c3ccccc23)cc1 10.1016/j.bmcl.2005.02.070
118626208 165001 0 None -416 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241830 165001 0 None -416 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
2232766 160824 7 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
CHEMBL4126145 160824 7 None -47 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr
ChEMBL 297 7 0 2 4.9 c1ccc2c(OCCCCCN3CCCCC3)cccc2c1 10.1016/j.bmc.2018.04.023
126720445 161666 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4162914 161666 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)nccc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
155558380 174195 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2ccc(C3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4561144 174195 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 342 3 1 3 2.9 O=S(=O)(c1ccccc1)N1Cc2ccc(C3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
163409061 191591 2 None -74 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 456 8 1 6 3.2 O=C(NCCCCCCn1nc2ccccn2c1=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5204274 191591 2 None -74 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 456 8 1 6 3.2 O=C(NCCCCCCn1nc2ccccn2c1=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
86288950 112146 0 None -8511 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233666 112146 0 None -8511 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302931 112146 0 None -8511 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 452 8 0 4 3.9 CN1C(=O)N(CCCCCN2CCN(c3ccccc3F)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
162650377 179453 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 250 3 0 2 3.8 CN(C)c1cccc2c1ccn2Cc1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4747483 179453 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 250 3 0 2 3.8 CN(C)c1cccc2c1ccn2Cc1ccccc1 10.1016/j.ejmech.2020.112916
4543 169982 36 None -9 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -9 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -9 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
71574210 85856 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312934 85856 0 None -21 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
181743 177997 3 None -128 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177997 3 None -128 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
11681803 154569 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 348 2 2 3 4.1 CNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL401969 154569 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 348 2 2 3 4.1 CNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
71451457 81015 0 None -16 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 394 8 1 5 3.3 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccs2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159470 81015 0 None -16 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 394 8 1 5 3.3 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccs2)C1 10.1016/j.ejmech.2012.07.043
162648387 179297 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 594 13 1 5 7.3 C#CCNC1CCc2c(OCCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4745652 179297 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 594 13 1 5 7.3 C#CCNC1CCc2c(OCCCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
74763017 113220 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
CHEMBL3323289 113220 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 379 1 1 4 2.6 CN1CCc2ccc(N3C(=O)CSC34C(=O)Nc3ccccc34)cc2CC1 10.1016/j.bmcl.2014.06.081
197033 197473 58 None -3 8 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1021/jm5003952
CHEMBL589390 197473 58 None -3 8 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1021/jm5003952
9952250 203252 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1021/jm010943m
CHEMBL76466 203252 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1021/jm010943m
197033 197473 58 None -3 8 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptorBinding affinity to human recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 197473 58 None -3 8 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptorBinding affinity to human recombinant 5HT6 receptor
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
2726 906 64 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -10 72 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
155554462 174029 0 None 7 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 316 4 1 7 1.5 CN1CCN(c2nc(N)nc(CSc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4557247 174029 0 None 7 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 316 4 1 7 1.5 CN1CCN(c2nc(N)nc(CSc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
145950947 162233 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 3 1 5 2.5 Cc1cccc(Cn2c(C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172073 162233 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 3 1 5 2.5 Cc1cccc(Cn2c(C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
3643745 93609 5 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 370 7 1 6 3.1 Cc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
CHEMBL248846 93609 5 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 370 7 1 6 3.1 Cc1ccccc1OCCNc1cc(N2CCN(C)CC2)ccc1[N+](=O)[O-] 10.1016/j.bmcl.2007.09.016
44403087 132609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370306 132609 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
164620867 185060 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864448 185060 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
53327999 111207 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286590 111207 0 None 33 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 383 3 1 6 2.2 COc1ccccc1S(=O)(=O)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
164616796 184304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4852840 184304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
44405369 72091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 4 2 5 3.0 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL198797 72091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 4 2 5 3.0 CNc1cc(NC)c2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.bmcl.2005.08.059
44474470 13947 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL1197489 13947 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
CHEMBL573981 13947 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 414 4 4 6 1.4 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N/NC(=N)N)CC4)cc21 10.1021/jm900796p
56944190 111608 0 None -5 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 499 8 1 5 5.2 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289994 111608 0 None -5 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 499 8 1 5 5.2 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
66801120 111622 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 7 1 5 5.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3290007 111622 0 None -8 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 7 1 5 5.3 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
57414520 131172 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1ccc(-n2cccn2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692913 131172 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 413 3 1 6 3.8 O=S(=O)(c1ccc(-n2cccn2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
57414658 131188 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 348 2 1 5 3.0 O=S(=O)(c1cccnc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692929 131188 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 348 2 1 5 3.0 O=S(=O)(c1cccnc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25263345 173204 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL453732 173204 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
49799685 10849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL1173209 10849 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 493 4 1 8 5.3 CC12CC3CC(C)(C1)CC(Nc1nc4c(S(=O)(=O)c5ccccc5)nnn4c4ccsc14)(C3)C2 10.1016/j.bmc.2010.05.051
CHEMBL5087742 213342 0 None -6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2csc3ccccc23)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
162652285 179695 0 None -15 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
CHEMBL4750664 179695 0 None -15 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 399 7 1 5 3.1 Cc1cccc(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)c1 10.1016/j.ejmech.2020.112149
56595670 65346 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834332 65346 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 338 5 1 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC(CC)C=N1 10.1021/jm200466r
164611003 184762 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 184762 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
11833220 16586 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 292 5 1 2 3.5 CN(C)CCc1cccc2[nH]c(C(=O)c3ccccc3)cc12 10.1021/jm010943m
CHEMBL124382 16586 2 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 292 5 1 2 3.5 CN(C)CCc1cccc2[nH]c(C(=O)c3ccccc3)cc12 10.1021/jm010943m
4713248 206170 3 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 206170 3 None -2 3 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
145964159 163777 0 None -56 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4212435 163777 0 None -56 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 273 3 2 4 2.6 C[C@@H]1SC(c2ccccc2O)=N[C@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
71463518 84874 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 237 3 2 2 2.7 NCCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260376 84874 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 237 3 2 2 2.7 NCCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
15256441 180435 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4759121 180435 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 287 3 0 4 2.9 COc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
164615095 184364 0 None -204 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 414 7 0 6 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4853700 184364 0 None -204 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 414 7 0 6 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2021.128028
155545526 172827 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4528162 172827 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
134152583 152643 0 None -10 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2cccnc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3976948 152643 0 None -10 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 530 10 1 5 4.8 O=C(CCOCCN1CCN(c2cccnc2-c2ccc(F)cc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
155554246 174378 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 315 6 3 1 4.5 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)[nH]2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4565614 174378 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 315 6 3 1 4.5 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)[nH]2)cc1 10.1016/j.ejmech.2019.111857
72198014 89388 0 None -8 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 484 7 2 4 4.8 COc1ccc2[nH]cc(C3CCN(CCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
CHEMBL2377443 89388 0 None -8 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 484 7 2 4 4.8 COc1ccc2[nH]cc(C3CCN(CCCN4C(=O)CC(c5c[nH]c6ccccc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2013.02.033
57393877 68087 0 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917350 68087 0 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 401 7 1 5 3.4 O=S(=O)(NCCCCN1CCc2sccc2C1)c1ccc2cccnc2c1 10.1016/j.bmc.2011.09.044
137652210 156954 0 None 19 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 375 3 0 5 4.0 O=CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4079631 156954 0 None 19 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 375 3 0 5 4.0 O=CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
4723679 171188 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 384 6 2 2 6.1 Clc1cc(Cl)cc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4467393 171188 4 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 384 6 2 2 6.1 Clc1cc(Cl)cc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
49782362 16996 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 783 15 2 9 7.6 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256250 16996 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 783 15 2 9 7.6 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
155543223 172726 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2c(N3CCN(C4CCC4)CC3)cccc21 10.1016/j.bmcl.2016.07.055
CHEMBL4525992 172726 0 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1CCc2c(N3CCN(C4CCC4)CC3)cccc21 10.1016/j.bmcl.2016.07.055
164618208 184803 0 None -2630 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 467 6 0 5 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4860626 184803 0 None -2630 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 467 6 0 5 3.7 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
71456781 81016 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159471 81016 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 3.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cccs1 10.1016/j.ejmech.2012.07.043
164610188 184472 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4855393 184472 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
145974189 164074 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 434 9 1 4 4.2 CC(C)c1ccccc1OCCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
CHEMBL4216126 164074 0 None -8 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 434 9 1 4 4.2 CC(C)c1ccccc1OCCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2017.03.057
117209864 185452 1 None -1 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4870675 185452 1 None -1 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
145962275 161107 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 373 3 1 3 5.3 Clc1cccc(Cn2cc(C3=CCNCC3)c3ccc4cccnc4c32)c1 10.1016/j.bmc.2018.05.033
CHEMBL4130316 161107 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 373 3 1 3 5.3 Clc1cccc(Cn2cc(C3=CCNCC3)c3ccc4cccnc4c32)c1 10.1016/j.bmc.2018.05.033
58258806 127443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664790 127443 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cccnc45)ccc31)C1CCC(C2)N1 nan
44389010 62939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179173 62939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44395499 66592 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 318 4 1 4 2.6 NCCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
CHEMBL186585 66592 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 318 4 1 4 2.6 NCCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
23872163 109990 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 385 6 1 5 2.9 CC(=O)Nc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL324766 109990 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 385 6 1 5 2.9 CC(=O)Nc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3ccccc32)cc1 10.1016/s0960-894x(03)00612-7
53325577 59842 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642874 59842 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739700 59842 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44389010 62939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL179173 62939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 388 3 1 4 4.4 O=S(=O)(c1ccc2ccccc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
22015412 179946 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4753562 179946 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
11638206 93907 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 4 0 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(Oc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250677 93907 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 313 4 0 5 3.1 CN1CCN(c2ccc([N+](=O)[O-])c(Oc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
164611003 184762 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 184762 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164622054 185612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 0 5 4.4 CN(CCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1)Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4872905 185612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 420 8 0 5 4.4 CN(CCOc1cccc2c1ccn2S(=O)(=O)c1ccccc1)Cc1ccccc1 10.1016/j.ejmech.2021.113792
49780586 16998 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 9 6.1 COc1ccc(N(S(=O)(=O)c2sc3ccc(Cl)cc3c2C)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256252 16998 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 684 8 1 9 6.1 COc1ccc(N(S(=O)(=O)c2sc3ccc(Cl)cc3c2C)S(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
49836719 18503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
CHEMBL1277286 18503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 2 5 2.1 Cc1ccc(S(=O)(=O)c2n[nH]c3cc(N4CCNCC4)ccc23)cc1 10.1021/jm1007825
57396813 71201 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None -5 5 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
66800909 111578 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 8 3.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3289965 111578 0 None -13 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 8 3.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
56944082 111586 0 None -269 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289972 111586 0 None -269 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 8 1 6 3.5 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68108968 131154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 2 1 4 4.3 CC1(C)NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692895 131154 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 375 2 1 4 4.3 CC1(C)NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
24967096 83611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207376 83611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
56595669 65322 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834243 65322 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 322 4 1 3 2.0 CCN/C(=N\S(=O)(=O)c1cccc(C)c1)N1CC(CC)C=N1 10.1021/jm200466r
162666034 181729 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4784228 181729 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
9983033 155585 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4063362 155585 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(Br)ccc32)cc1 10.1021/acs.jmedchem.6b01662
44397550 70848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL188285 70848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL195621 70848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
24855787 65303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834221 65303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1ccccc1Cl)N1CC(CC)C=N1 10.1021/jm200466r
71463519 84875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 265 4 1 2 3.3 CN(C)CCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260377 84875 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 265 4 1 2 3.3 CN(C)CCc1c(-c2ccccc2)[nH]c2ccncc12 10.1007/s00044-004-0121-8
1984087 161747 10 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 3 5.3 COc1cc(CNCCC2=CCCCC2)ccc1OCc1ccccc1 10.1016/j.ejmech.2018.04.010
CHEMBL4164250 161747 10 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 9 1 3 5.3 COc1cc(CNCCC2=CCCCC2)ccc1OCc1ccccc1 10.1016/j.ejmech.2018.04.010
594590 72505 89 None -39 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL200234 72505 89 None -39 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1016/j.bmcl.2005.08.059
90645147 111684 0 None -13 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL3290576 111684 0 None -13 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 304 2 1 6 1.5 CN1CCN(c2nc(N)nc(-c3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
71456784 81037 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159492 81037 0 None -26 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 440 8 1 4 3.9 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
44403085 133027 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.8 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370935 133027 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 326 2 1 4 2.8 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNC3)cc1 10.1016/j.bmcl.2005.07.028
73213195 103980 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 103980 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
164612518 184812 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4860719 184812 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
73213195 103980 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 103980 0 None -9 12 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL508338 188379 0 None -95 6 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL None None None None nan
57398619 71222 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949962 71222 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963099 71222 0 None -24 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
71451454 81000 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 398 8 1 5 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159456 81000 0 None -3 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 398 8 1 5 3.0 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
127039755 136130 0 None -45 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 470 8 1 4 4.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1039/C5MD00166H
CHEMBL3740055 136130 0 None -45 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 470 8 1 4 4.8 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1039/C5MD00166H
16718916 182079 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL478896 182079 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3cccc4ccccc34)ccc2C1 10.1021/jm8009469
168292411 191293 0 None -34 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 8 2.8 Nc1nc(NCCc2c[nH]c3ccccc23)nc(NCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5199820 191293 0 None -34 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 8 2.8 Nc1nc(NCCc2c[nH]c3ccccc23)nc(NCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
137648205 157335 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 370 4 0 6 2.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ncccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4083953 157335 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 370 4 0 6 2.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ncccc23)CC1 10.1021/acs.jmedchem.6b01662
24968180 83605 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(Br)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207367 83605 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 489 5 0 5 4.5 CC(C)c1ccc(S(=O)(=O)n2cc(Br)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
117209971 185903 1 None -5 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 185903 1 None -5 5 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
168283609 190643 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 418 10 5 8 3.1 COc1ccccc1NCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5190020 190643 0 None 1 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 418 10 5 8 3.1 COc1ccccc1NCCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
9841077 9398 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL112024 9398 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 344 5 1 5 2.7 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(O)cc12 10.1016/s0960-894x(03)00612-7
137635185 155316 0 None 60 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 382 6 0 5 4.0 CCN(CC)CC1=Cc2cn(S(=O)(=O)c3ccccc3)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4060194 155316 0 None 60 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 382 6 0 5 4.0 CCN(CC)CC1=Cc2cn(S(=O)(=O)c3ccccc3)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
16116897 59811 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642876 59811 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739544 59811 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCNCC1 10.1016/j.bmc.2010.10.033
137658424 159173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4104479 159173 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3cccc(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
155519102 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4447416 169787 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 348 4 1 7 2.0 CC(Oc1ccccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
2771410 154447 35 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 2 5 2.6 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL401294 154447 35 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 5 2 5 2.6 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
155550580 173710 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.5 CCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4549734 173710 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.5 CCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
57393365 71206 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949773 71206 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963026 71206 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 351 2 1 4 2.6 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
68109417 131148 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cn[nH]c2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692889 131148 0 None - 1 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cn[nH]c2)c2oc3c(c2c1)CNCC3 nan
137640966 156534 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Cl)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4074234 156534 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Cl)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
25024148 62624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 5 0 5 3.7 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785058 62624 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 5 0 5 3.7 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
11574113 94304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 3 2 3 4.5 CCNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL253095 94304 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 3 2 3 4.5 CCNc1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
58158707 138519 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786087 138519 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 374 3 2 4 2.1 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ncc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
16019573 10892 10 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173579 10892 10 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 543 5 1 10 4.3 O=S(=O)(c1ccc(Br)cc1)c1nnn2c1nc(NCc1ccc3c(c1)OCO3)c1sccc12 10.1016/j.bmc.2010.05.051
9921064 126657 18 None 8 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counterDisplacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counter
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
CHEMBL365751 126657 18 None 8 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counterDisplacement of [3H] lysergic acid diethylamide from rat 5-HT6 receptor transfected in HEK293 cells after 60 mins by scintillation counter
ChEMBL 236 3 1 1 3.2 Cc1[nH]c2ccc(Cl)cc2c1CCN(C)C 10.1021/acs.jmedchem.5b00179
53327976 111202 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286586 111202 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
25263352 183549 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL482748 183549 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 4 1 4 3.5 Cc1ccc(S(=O)(=O)Oc2cccc(C3CCNCC3)c2C)cc1 10.1016/j.bmcl.2009.03.077
16222654 81646 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165561 81646 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
44438708 92975 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 0 4 2.3 CCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL245806 92975 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 6 0 4 2.3 CCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
56944951 156096 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4069237 156096 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 479 7 2 3 5.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
155538716 172689 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 434 3 0 6 3.8 CC(=O)N1CCCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4524906 172689 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 434 3 0 6 3.8 CC(=O)N1CCCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
1524 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 2150 89 None -257 51 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
127026750 137152 0 None -14 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 O=S(=O)(NC1CCN(CCOc2ccccc2C2CCCC2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3758591 137152 0 None -14 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 O=S(=O)(NC1CCN(CCOc2ccccc2C2CCCC2)CC1)c1cccc(F)c1 10.1016/j.ejmech.2015.11.040
134147935 149157 0 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3947670 149157 0 None -26 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 487 10 1 6 3.6 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
168290061 190740 0 None -56 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 424 8 3 8 2.7 Nc1nc(N)nc(NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5191557 190740 0 None -56 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 424 8 3 8 2.7 Nc1nc(N)nc(NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
90654672 109604 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 9 1 5 3.5 CSc1ccccc1N1CCN(CCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3235744 109604 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 480 9 1 5 3.5 CSc1ccccc1N1CCN(CCCCCC(=O)N2Cc3ccccc3C[C@H]2C(N)=O)CC1 10.1016/j.ejmech.2014.12.041
44403078 71068 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 4 1 5 5.3 Cc1c(S(=O)(=O)n2cc(C[C@H]3CCCN3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL195922 71068 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 4 1 5 5.3 Cc1c(S(=O)(=O)n2cc(C[C@H]3CCCN3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
57392612 70410 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70410 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
11849198 138527 30 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 248 3 2 3 2.1 Nc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL378618 138527 30 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 248 3 2 3 2.1 Nc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
168279047 190591 0 None -2818 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 437 8 0 8 2.7 O=c1n(CCCCCCN2CCN(c3cccc4c3OCCO4)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5189101 190591 0 None -2818 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 437 8 0 8 2.7 O=c1n(CCCCCCN2CCN(c3cccc4c3OCCO4)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
145965668 163562 0 None -11 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3Cl)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4209807 163562 0 None -11 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3Cl)CC1)C2 10.1016/j.bmcl.2018.06.019
168281784 190353 0 None -47 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 429 8 0 6 4.0 O=c1n(CCCCCCN2CCN(c3cccc4ccccc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5185787 190353 0 None -47 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 429 8 0 6 4.0 O=c1n(CCCCCCN2CCN(c3cccc4ccccc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
44403102 71388 0 None -102 6 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196598 71388 0 None -102 6 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
90654858 112203 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233678 112203 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304355 112203 0 None -6 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 550 9 0 4 6.2 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2014.01.065
139488606 170190 1 None -724 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(I)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4452569 170190 1 None -724 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 355 2 1 2 3.8 CCn1cncc1-c1c[nH]c2ccc(I)c(F)c12 10.1016/j.ejmech.2019.03.017
137630865 160573 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4073685 160573 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4117161 160573 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3cccc(Br)c3)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
155554020 174869 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2ccc(N3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4576668 174869 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 343 3 1 4 1.8 O=S(=O)(c1ccccc1)N1Cc2ccc(N3CCNCC3)cc2C1 10.1016/j.bmcl.2016.07.055
44386772 12915 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 352 3 1 5 3.6 COc1ccc2c(c1)c1ccccc1n2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL1189868 12915 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 352 3 1 5 3.6 COc1ccc2c(c1)c1ccccc1n2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.01.071
44388987 62169 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc([N+](=O)[O-])ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178123 62169 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc([N+](=O)[O-])ccc32)cc1 10.1016/j.bmcl.2004.10.064
44397119 12305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1185807 12305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL433765 12305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
4376990 192407 4 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192407 4 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192407 4 None -11 11 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
6918748 126306 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL365471 126306 2 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
44438726 150002 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 292 5 0 2 4.1 Cc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL395465 150002 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 292 5 0 2 4.1 Cc1ccc(Cn2cc(CCN(C)C)c3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
44567986 182413 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
CHEMBL479349 182413 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
155562997 174665 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL4571862 174665 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccccc23)CC1 10.1016/j.ejmech.2019.111736
137643504 157863 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090168 157863 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3Cl)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
53327976 111202 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286586 111202 0 None 38 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 371 2 1 5 2.4 O=S(=O)(c1ccc(F)cc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
155534153 175676 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4469860 175676 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594878 175676 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 366 4 2 5 3.4 CCc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
66801263 111584 0 None -40 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289970 111584 0 None -40 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
68109159 131163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68116317 131189 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 416 2 1 5 4.0 O=S(=O)(c1cncc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692930 131189 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 416 2 1 5 4.0 O=S(=O)(c1cncc(C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
71462331 81650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 468 3 0 4 4.3 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165565 81650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 468 3 0 4 4.3 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2)C1 10.1016/j.bmcl.2012.06.002
24965681 83610 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207375 83610 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 399 5 0 6 2.6 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
137634934 155260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1cccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4059662 155260 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1cccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
129103315 166569 0 None -3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4290311 166569 0 None -3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 477 7 1 5 4.9 O=C1CCc2cc(C(O)CCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
137633065 155993 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 6 0 6 4.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)c(Cl)n2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4068056 155993 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 6 0 6 4.4 COc1ccc2c(c1)c(CN1CCN(C)CC1)c(Cl)n2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
11849791 77686 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 262 4 2 3 1.9 NCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL209909 77686 3 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 262 4 2 3 1.9 NCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
2894562 154277 12 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 376 7 2 6 3.1 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
CHEMBL400349 154277 12 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 376 7 2 6 3.1 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCOc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
127046815 139493 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 518 8 0 7 4.9 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(OCc4ccccc4)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800150 139493 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 518 8 0 7 4.9 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(OCc4ccccc4)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
71463521 84877 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 217 4 1 2 2.2 CCc1[nH]c2ccncc2c1CCN(C)C 10.1007/s00044-004-0121-8
CHEMBL2260379 84877 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 217 4 1 2 2.2 CCc1[nH]c2ccncc2c1CCN(C)C 10.1007/s00044-004-0121-8
168269719 189418 0 None 2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 444 7 3 8 2.9 COc1ccccc1N1CCN(c2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5171456 189418 0 None 2 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 444 7 3 8 2.9 COc1ccccc1N1CCN(c2nc(N)nc(NCCc3c[nH]c4ccccc34)n2)CC1 10.1016/j.ejmech.2021.113931
57401515 68056 0 None -4466 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 498 8 0 5 4.0 COc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL1916745 68056 0 None -4466 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 498 8 0 5 4.0 COc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
145983139 165311 0 None -72 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249179 165311 0 None -72 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
90654842 112147 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
CHEMBL3233670 112147 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
CHEMBL3302936 112147 0 None -66 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1cccc(N2CCN(CCCCCN3C(=O)N(Cc4ccccc4)C(=O)C3(C)C)CC2)c1 10.1016/j.ejmech.2014.01.065
164614157 184570 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 3 5.2 Cc1cccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4857018 184570 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 370 8 1 3 5.2 Cc1cccc(CNCCOc2cccc3c2ccn3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
44446213 94487 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL254330 94487 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
16763549 117438 9 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 342 5 1 5 2.8 COCCn1c(C)c(C)c(S(=O)(=O)c2ccc(Cl)cc2)c1N 10.1016/j.bmcl.2015.03.049
CHEMBL3403344 117438 9 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 342 5 1 5 2.8 COCCn1c(C)c(C)c(S(=O)(=O)c2ccc(Cl)cc2)c1N 10.1016/j.bmcl.2015.03.049
132938109 163751 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 500 9 2 5 4.2 O=S(=O)(NC1CCN(CC(O)COc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2017.03.057
CHEMBL4212199 163751 0 None -8 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 or CHO-K1 cells after 1 hr by microbeta counting analysis
ChEMBL 500 9 2 5 4.2 O=S(=O)(NC1CCN(CC(O)COc2ccccc2-c2ccccc2)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2017.03.057
11653679 180609 1 None -44 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 180609 1 None -44 11 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
139488539 170858 0 None -186 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 307 2 1 2 4.0 CCn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4462820 170858 0 None -186 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 307 2 1 2 4.0 CCn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
161 743 3 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 743 3 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 743 3 None -12 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
168292233 191264 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 4.2 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5199228 191264 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 4.2 O=c1n(CCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
145984807 165223 0 None -602 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4247275 165223 0 None -602 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cncc5ccccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
42631003 197937 10 None -10 8 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/jm5003952
CHEMBL592752 197937 10 None -10 8 Human 8.5 pKi = 8.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 304 3 0 2 4.2 Cc1ccc2c(c1)c1c(n2CCc2ccccc2)CCN(C)C1 10.1021/jm5003952
58258861 127411 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 2 1 4 4.3 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664757 127411 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 2 1 4 4.3 Cc1cc(S(=O)(=O)c2cccc(Cl)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
89888370 128481 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 5 1 6 4.0 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669680 128481 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 448 5 1 6 4.0 COc1cc(S(=O)(=O)c2cccc(OC(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2005.01.031
11818252 174741 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.05.076
CHEMBL457351 174741 1 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2004.05.076
44388951 62200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL178234 62200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 378 3 1 5 4.0 O=S(=O)(c1ccc(Cl)s1)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
44388956 62757 0 None 38 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178870 62757 0 None 38 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 389 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
11361090 63974 0 None 32 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181066 63974 0 None 32 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 383 4 2 6 2.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2004.10.064
44388950 122089 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL360234 122089 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 387 3 2 5 3.5 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2004.10.064
44389074 122796 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL361572 122796 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 374 3 1 4 3.5 O=S(=O)(c1ccc(F)cc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
44401277 69924 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 263 5 1 1 4.0 CNCCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL194174 69924 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 263 5 1 1 4.0 CNCCC1=CC(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
9867475 17829 0 None 21 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 17829 0 None 21 9 Human 8.5 pKi = 8.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
11723168 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
CHEMBL94422 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmc.2009.08.006
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptorBinding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
11976 907 54 None -3 23 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
667467 907 54 None -3 23 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
CHEMBL908 907 54 None -3 23 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
DB01239 907 54 None -3 23 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1021/jm030030n
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm030030n
23815447 9751 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 8 1 6 4.1 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL114048 9751 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 449 8 1 6 4.1 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccc(N)cc1 10.1016/s0960-894x(03)00612-7
146680920 171308 0 None 50 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4469309 171308 0 None 50 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cncc2ccccc12 10.1021/acsmedchemlett.6b00056
155566191 175166 0 None 13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4583082 175166 0 None 13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
90468813 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2019.06.022
CHEMBL4125735 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2019.06.022
90468813 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
CHEMBL4125735 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
90468813 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4125735 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469114 183840 0 None 257 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4846153 183840 0 None 257 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469183 184913 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4862354 184913 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1cccc(C(F)(F)F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469115 185260 2 None 36 17 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185260 2 None 36 17 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
90469187 185426 0 None 251 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 1 6 3.1 Cc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
CHEMBL4870374 185426 0 None 251 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 406 3 1 6 3.1 Cc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
164626889 185995 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 449 11 2 6 3.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4878361 185995 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 449 11 2 6 3.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
164627505 185997 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4878383 185997 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 483 11 2 6 4.3 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113783
162646407 179043 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4742804 179043 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 419 4 1 7 2.9 CC(C)c1nc2c(N3CCNCC3)nccc2n1S(=O)(=O)c1cccc(Cl)c1 10.1021/acs.jmedchem.0c02009
162646981 179136 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 361 3 1 7 1.2 O=S(=O)(c1cccc(F)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4743983 179136 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 361 3 1 7 1.2 O=S(=O)(c1cccc(F)c1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
162657990 180496 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4759927 180496 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1cnc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
10115005 71340 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL196466 71340 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 452 5 1 7 4.2 Cc1nc(N)sc1S(=O)(=O)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403097 72101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL198827 72101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 480 4 0 4 4.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(I)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10136185 126658 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
CHEMBL365753 126658 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 3 0 4 4.6 CN1CCC(c2cn(S(=O)(=O)c3ccc(Cl)c(Cl)c3)c3ccccc23)C1 10.1016/j.bmcl.2005.07.028
9902533 133079 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371292 133079 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 340 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10199819 133085 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371318 133085 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 380 3 1 5 4.1 O=S(=O)(c1ccc(Cl)s1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403103 140778 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL383373 140778 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 4 1 5 3.1 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403047 167864 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL434932 167864 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
276 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
5312149 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
CHEMBL431298 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
90468813 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4125735 160788 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hrDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
ChEMBL 426 4 2 6 3.9 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCNC3)nc3ccccc3c21 10.1016/j.bmc.2018.05.033
9824783 176029 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45977 176029 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 445 3 0 5 4.7 O=S(=O)(c1ccc2ccccc2c1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
164618065 184770 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 408 8 1 4 3.6 O=S(=O)(c1ccccc1)N1CCc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4860124 184770 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 408 8 1 4 3.6 O=S(=O)(c1ccccc1)N1CCc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
164623617 184906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 410 8 1 6 3.9 Cc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)o1 10.1016/j.ejmech.2021.113792
CHEMBL4862289 184906 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 410 8 1 6 3.9 Cc1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)o1 10.1016/j.ejmech.2021.113792
164618728 184942 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4862752 184942 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 450 10 1 6 4.4 CCOc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164621287 184964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccncc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863037 184964 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 407 8 1 6 3.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccncc3)cccc21 10.1016/j.ejmech.2021.113792
46227396 199955 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
CHEMBL605938 199955 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 420 4 2 6 3.4 O=S(=O)(Nc1ccc2c(c1)C(C1CCNC1)=CC2)c1c(Cl)nc2sccn12 10.1016/j.bmc.2009.08.006
11818252 174741 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1021/jm8009469
CHEMBL457351 174741 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 277 5 0 1 4.4 CN(C)CCC1=CC(Cc2ccccc2)c2ccccc21 10.1021/jm8009469
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm8009469
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm8009469
155566665 175332 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 500 7 2 6 4.8 COc1ccc2c(c1)c(-c1[nH]c(NC(=O)Cc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4586990 175332 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 500 7 2 6 4.8 COc1ccc2c(c1)c(-c1[nH]c(NC(=O)Cc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155560943 175993 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4574931 175993 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4597364 175993 0 None 223 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 382 4 2 6 3.2 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
127047680 139387 0 None 562 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 5 1 6 4.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCNCC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799529 139387 0 None 562 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 5 1 6 4.0 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCNCC3)nc21 10.1016/j.bmcl.2016.04.024
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/j.bmcl.2007.11.045
16718922 196543 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
CHEMBL575310 196543 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 434 4 1 6 3.7 CN1CCC(C2=CCc3ccc(NS(=O)(=O)c4c(Cl)nc5sccn45)cc32)C1 10.1021/jm900796p
11177383 200047 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606549 200047 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 411 6 2 3 4.7 CC(C)c1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
11407867 200077 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
CHEMBL606704 200077 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
11223004 200528 0 None 4 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 200528 0 None 4 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
11440676 200529 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
CHEMBL609743 200529 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)cc1 10.1021/jm049243i
11418830 200611 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.6 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)c(Cl)c1 10.1021/jm049243i
CHEMBL610257 200611 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.6 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(Cl)c(Cl)c1 10.1021/jm049243i
68115633 131196 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1ccc(F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692937 131196 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 365 2 1 4 3.7 O=S(=O)(c1ccc(F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115804 131204 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692945 131204 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
276 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
5312149 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
CHEMBL431298 3457 45 None 81 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm5003759
25024724 62632 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785065 62632 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(Cl)cc3)c2)CC1 10.1021/ml100101u
25123014 198747 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598229 198747 0 None 6 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
9800707 202798 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL72574 202798 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(Cl)cc1 10.1016/s0960-894x(00)00453-4
11723168 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
11723168 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL94422 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL94422 205761 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 314 4 0 4 2.9 CN(C)Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
16117281 59828 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642880 59828 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739648 59828 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 356 4 3 5 2.6 O=S(=O)(c1ccccc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
23624309 176159 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460195 176159 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
68109159 131163 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692904 131163 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 3 3.9 [O-][S+](c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115765 131209 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692950 131209 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@@H](O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
25024725 62633 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
CHEMBL1785066 62633 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1016/s0960-894x(00)00597-7
17940243 45214 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3cc(Br)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL152806 45214 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 465 4 1 5 3.0 COc1ccc(S(=O)(=O)N2CCCc3cc(Br)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369828 47200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 477 5 2 5 3.5 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154534 47200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 477 5 2 5 3.5 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354557 47531 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL154842 47531 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Cl)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9803937 111871 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cccc2c(Cl)cccc12 10.1016/s0960-894x(01)00558-3
CHEMBL329482 111871 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1cccc2c(Cl)cccc12 10.1016/s0960-894x(01)00558-3
10769116 158006 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 553 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2c(F)c(Br)cc(F)c2Br)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL409160 158006 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 553 5 1 5 4.1 COc1ccc(NS(=O)(=O)c2c(F)c(Br)cc(F)c2Br)cc1N1CCN(C)CC1 10.1021/jm980532e
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 10.1021/jm050247c
44398568 124018 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 1 4 2.3 NCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
CHEMBL364039 124018 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 286 3 1 4 2.3 NCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
9927441 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
CHEMBL93868 205662 0 None 6 9 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm050247c
10182109 71407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 445 3 1 6 4.5 Cc1c(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.06.107
CHEMBL196644 71407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 445 3 1 6 4.5 Cc1c(S(=O)(=O)n2ccc3c(N4CCNCC4)cccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.06.107
22557292 153038 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1ccccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL398035 153038 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 2.3 O=S(=O)(c1ccccc1Cl)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
58258866 128452 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 4 5.0 CC(C)N1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
CHEMBL3669651 128452 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 4 5.0 CC(C)N1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccc5[nH]ccc5c4)cc13)C2 nan
7185123 10577 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170673 10577 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 413 4 1 8 3.9 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44435653 146867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL392976 146867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880707 8453 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1094370 8453 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 360 3 1 4 3.7 O=S(=O)(c1cccc(Cl)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
10405986 18602 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1278092 18602 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 356 3 1 6 1.8 Cn1nc(S(=O)(=O)c2ccccc2)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
44591611 183823 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL484593 183823 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
25024322 62622 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 5 0 5 3.2 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1785056 62622 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 401 5 0 5 3.2 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(F)cc3)c2)CC1 10.1021/ml100101u
44435653 146867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL392976 146867 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 4 0 6 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)s3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162674129 182631 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4795995 182631 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 441 7 1 6 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2s1 10.1016/j.ejmech.2020.112149
24965329 83623 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207388 83623 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
44476607 81940 2 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172192 81940 2 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.Radioligand Binding Assay: The screening of the disclosed compounds for their potential ability to interact with serotonin 5-HT6 receptors was carried out b the method of radioligand binding.
ChEMBL 357 3 1 7 1.6 CNc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
58258828 127410 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664756 127410 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258756 127435 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127435 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
58258776 128484 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669683 128484 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44413494 138802 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2006.04.094
CHEMBL379273 138802 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 302 3 1 5 2.5 COc1cccc2c1ccn2S(=O)(=O)c1ccc(N)cc1 10.1016/j.bmcl.2006.04.094
44435624 88674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236541 88674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44293023 180996 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.5 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
CHEMBL47691 180996 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.5 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
45484322 197127 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL583389 197127 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 369 5 0 6 3.1 CN(C)CCn1cc(S(=O)(=O)c2ccc(Cl)s2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263314 184203 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(OCc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485147 184203 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(OCc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
56944384 111629 0 None -4 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3290014 111629 0 None -4 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 521 8 1 6 5.8 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
10276057 60335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 455 8 2 3 5.7 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4c(Cl)cccc34)cc12 10.1021/jm049615n
CHEMBL176028 60335 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 455 8 2 3 5.7 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4c(Cl)cccc34)cc12 10.1021/jm049615n
68116201 131170 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1OC(F)(F)F nan
CHEMBL3692911 131170 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1OC(F)(F)F nan
57414526 131179 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692920 131179 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115693 131200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1cccc(C(O)C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692941 131200 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1cccc(C(O)C(F)(F)F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
44435624 88674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236541 88674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 389 4 0 5 3.8 CCN1CCC(n2cc(S(=O)(=O)c3cccc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
25024729 62602 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 439 4 0 5 3.6 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2F)CC1 10.1021/ml100101u
CHEMBL1784912 62602 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 439 4 0 5 3.6 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(F)cc2F)CC1 10.1021/ml100101u
44435643 147066 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393107 147066 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258857 128460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128460 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
53316820 59819 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642872 59819 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739605 59819 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 3 5 2.8 NCCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
44435643 147066 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393107 147066 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 401 4 0 5 4.1 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
23653135 56387 3 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642412 56387 3 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 397 4 0 5 3.8 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2010.11.001
66801551 111631 0 None -16 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3290016 111631 0 None -16 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 519 8 1 6 5.6 Cc1c(S(=O)(=O)NCCCCN2CCC(c3noc4cc(F)ccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
68115817 131219 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(CO)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692960 131219 0 None - 1 Human 8.5 pKi = 8.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 405 4 1 5 3.7 CC(CO)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
16019292 10891 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1173578 10891 7 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 469 5 0 8 4.5 CN(Cc1ccccc1)c1nc2c(S(=O)(=O)c3cccc(Cl)c3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
16118796 59782 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642853 59782 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739217 59782 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2ccc(NCC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
66803595 159181 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4104622 159181 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 431 6 3 4 3.6 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
164622837 185316 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 479 12 2 7 3.6 COc1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
CHEMBL4868597 185316 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 479 12 2 7 3.6 COc1ccc(CNCCNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113783
164629021 185721 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 568 12 2 7 6.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4874513 185721 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 568 12 2 7 6.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
46880655 5477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1076684 5477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 0 4 3.5 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
164622459 185519 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4871678 185519 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1ccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
25263342 183567 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(COc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482937 183567 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 4 1 2 4.7 Cc1c(COc2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
10180527 63554 4 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL180425 63554 4 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
21071390 1956 48 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
8689 1956 48 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
CHEMBL3286580 1956 48 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
DB11957 1956 48 None -2 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2019.111857
25123013 198774 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL598443 198774 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 378 3 2 5 2.7 NC1CN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
67085396 127413 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 434 2 1 4 4.7 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664759 127413 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 434 2 1 4 4.7 Cc1cc(S(=O)(=O)c2cccc(C(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258754 128447 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128447 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
11545169 147118 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393158 147118 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
44293077 187236 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 3.8 O=S(=O)(c1ccc(F)cc1F)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL49598 187236 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 431 3 0 5 3.8 O=S(=O)(c1ccc(F)cc1F)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
10113909 185493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4871357 185493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 436 9 1 6 4.1 COc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
25122652 198978 0 None 134 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
CHEMBL599663 198978 0 None 134 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 420 3 2 5 3.8 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCC(N)CC4)cc23)c2ccccc12 10.1021/jm901674f
71456942 81637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2F)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165552 81637 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 402 4 0 5 3.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2F)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
11545169 147118 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393158 147118 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 369 4 0 5 3.5 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
52913106 127386 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664732 127386 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 1 4 3.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258754 128447 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669646 128447 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4cncc5ccccc45)ccc31)C1CCC(C2)N1 nan
58258841 128489 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669688 128489 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
9929665 66458 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL185958 66458 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 378 5 0 4 4.2 CN(C)CCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
44435628 147970 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL393830 147970 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
52913108 70417 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950762 70417 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
16222869 81629 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 452 4 0 5 4.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165544 81629 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 452 4 0 5 4.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435628 147970 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL393830 147970 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccccc1Cl)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
118712408 113674 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 351 3 1 3 4.1 O=S(=O)(c1ccccc1)c1ccc(C2CCNCC2)c2ccccc12 10.1021/jm5003952
CHEMBL3329443 113674 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 351 3 1 3 4.1 O=S(=O)(c1ccccc1)c1ccc(C2CCNCC2)c2ccccc12 10.1021/jm5003952
52913218 70418 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950763 70418 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
9841434 11644 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1181599 11644 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL183757 11644 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 352 3 1 4 3.1 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
4106 2466 16 None -7 33 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
5358812 2466 16 None -7 33 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
89 2466 16 None -7 33 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
CHEMBL93240 2466 16 None -7 33 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation countingDisplacement of [3H]-LSD from rat 5-Ht6 receptor expressed in HEK cells after 60 mins by liquid scintillation counting
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.bmcl.2016.03.036
44435639 88120 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235306 88120 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16750338 62300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783607 62300 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1016/j.bmcl.2009.04.108
71502676 117754 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 8 0 7 5.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc5ccoc5c4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409255 117754 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 8 0 7 5.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc5ccoc5c4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
134130753 141689 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(F)ccc1F 10.1016/j.ejmech.2016.09.008
CHEMBL3884325 141689 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysisDisplacement of [3H]lysergic acid diethylamide from human recombinant 5-HT6 receptor expressed in CHO cell membranes for 30 mins by liquid scintillation counting analysis
ChEMBL 484 7 0 7 4.4 O=c1ccc(OCCCN2CCC(c3noc4cc(F)ccc34)CC2)nn1-c1cc(F)ccc1F 10.1016/j.ejmech.2016.09.008
44435639 88120 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235306 88120 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 419 3 1 5 3.6 O=S(=O)(c1cccc(Br)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
44248103 62625 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1021/ml100101u
CHEMBL1785059 62625 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1021/ml100101u
44435647 88081 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL235117 88081 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162659494 180772 0 None -11 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4763085 180772 0 None -11 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
58258811 127437 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127437 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
44435647 88081 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235117 88081 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 423 3 0 5 4.4 CN1CCCC(n2cc(S(=O)(=O)c3cc(Cl)cc(Cl)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45487129 196129 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL572092 196129 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 3.4 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccc(Br)cc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
10297610 60721 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 10 2 3 5.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL176292 60721 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 10 2 3 5.8 CCCN(CCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
18354552 46438 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL153918 46438 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 537 5 2 5 4.1 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
18354572 47946 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3cc(C)c(C(F)(F)F)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL155234 47946 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 455 4 1 5 3.2 COc1ccc(S(=O)(=O)N2CCc3cc(C)c(C(F)(F)F)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44369364 49355 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 445 6 2 6 2.9 COc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
CHEMBL156610 49355 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 445 6 2 6 2.9 COc1ccc(C(F)(F)F)cc1NS(=O)(=O)c1ccc(OC)c(N2CCNCC2)c1 10.1016/s0960-894x(00)00597-7
17940121 50141 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cc(I)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157285 50141 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3cc(I)ccc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9825329 106963 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 456 4 2 6 4.2 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)oc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL318262 106963 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 456 4 2 6 4.2 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)oc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
18354590 119493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL350022 119493 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 493 5 2 5 4.0 COc1ccc(S(=O)(=O)Nc2cc(Br)cc(Cl)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10286610 120351 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm050247c
CHEMBL355905 120351 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 331 3 1 6 2.4 CSc1nc2ccccn2c(=N)c1S(=O)(=O)c1ccccc1 10.1021/jm050247c
134136921 142009 0 None 501 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3890882 142009 0 None 501 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
162650362 179433 0 None -19 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4747225 179433 0 None -19 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 435 7 1 5 4.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2ccccc2c1 10.1016/j.ejmech.2020.112149
46890219 6834 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 403 4 1 3 4.2 CC(C)(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1084359 6834 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 403 4 1 3 4.2 CC(C)(C)C(=O)NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21 10.1016/j.bmcl.2010.03.110
46889894 7015 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 4 1 5 2.3 CS(=O)(=O)c1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085115 7015 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 379 4 1 5 2.3 CS(=O)(=O)c1cccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
46890265 7342 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 1 4 2.2 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(N)(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1086572 7342 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 1 4 2.2 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)S(N)(=O)=O 10.1016/j.bmcl.2010.03.110
44441240 93281 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 404 3 1 4 3.7 CC1(C)CN(S(=O)(=O)c2ccccc2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL247121 93281 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 404 3 1 4 3.7 CC1(C)CN(S(=O)(=O)c2ccccc2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
44441239 149385 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 3 1 5 2.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
CHEMBL394949 149385 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 407 3 1 5 2.7 O=S(=O)(c1ccccc1)N1CCOc2c(N3CCCNCC3)cc(Cl)cc21 10.1016/j.bmcl.2006.12.093
10252272 141813 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 432 4 1 4 4.9 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)s3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL388674 141813 0 None 10 4 Human 8.4 pKi = 8.4 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 432 4 1 4 4.9 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)s3)cc2CC1 10.1016/j.bmcl.2006.10.036
168298632 192127 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysisDisplacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysis
ChEMBL 447 5 2 5 3.3 O=C(N[C@@H]1CCNC1)c1ccn(S(=O)(=O)c2cccc(Cl)c2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2021.128275
CHEMBL5220242 192127 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysisDisplacement of [3H] LSD from 5-HT6R in HEK293 cells assessed as inhibition constant incubated for 1 hr in presence of haloperidol by microbeta plate reader analysis
ChEMBL 447 5 2 5 3.3 O=C(N[C@@H]1CCNC1)c1ccn(S(=O)(=O)c2cccc(Cl)c2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2021.128275
16118928 59839 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642859 59839 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739697 59839 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCNCC3)cccc12 10.1016/j.bmc.2010.10.033
56944954 157024 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 445 7 3 4 4.0 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4080399 157024 0 None -15 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 445 7 3 4 4.0 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
155534201 171344 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4469870 171344 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 421 4 1 6 3.9 COc1ccc2c(c1)c(C1CCNCC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
137645924 157007 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
CHEMBL4080312 157007 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1cccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)c1 10.1016/j.ejmech.2017.04.033
118654517 189471 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5172390 189471 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 409 4 1 5 3.4 O=S(=O)(c1ccccc1F)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
145958161 161538 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4160888 161538 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 397 6 1 5 4.4 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137643783 157888 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4090395 157888 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
164623135 184965 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863079 184965 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccccc3Cl)cccc21 10.1016/j.ejmech.2021.113792
23655466 149614 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 368 4 1 4 3.7 NCCc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL395145 149614 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 368 4 1 4 3.7 NCCc1cn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c2ccccc12 10.1021/jm070521y
11559090 155021 0 None 60 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL404352 155021 0 None 60 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
23652861 56397 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 489 5 0 5 4.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642422 56397 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 489 5 0 5 4.9 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
7184886 10506 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
CHEMBL1170091 10506 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 373 4 1 8 3.0 CC(C)Nc1nc2c(S(=O)(=O)c3ccccc3)nnn2c2ccsc12 10.1016/j.bmc.2010.05.051
53317295 56406 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642431 56406 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3ccccc3Br)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
24966378 83617 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207382 83617 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
23652994 56401 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 445 5 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642426 56401 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 445 5 0 5 4.8 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2010.11.001
162669595 182162 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4790020 182162 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 489 7 1 6 5.0 Cc1c(S(=O)(=O)N[C@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(Cl)cc12 10.1016/j.ejmech.2020.112149
12051079 61036 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 4 1 3 4.1 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN 10.1016/j.bmcl.2004.01.071
CHEMBL176838 61036 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 4 1 3 4.1 COc1ccc2c(c1)c1c(n2Cc2ccccc2)CCCC1CN 10.1016/j.bmcl.2004.01.071
11820174 203168 8 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 202 3 1 1 2.6 Cc1[nH]c2ccccc2c1CCN(C)C 10.1021/jm990550b
CHEMBL7580 203168 8 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 202 3 1 1 2.6 Cc1[nH]c2ccccc2c1CCN(C)C 10.1021/jm990550b
66801052 158412 0 None -69 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4095979 158412 0 None -69 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
54580137 62212 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782366 62212 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
10873805 202988 2 None -83 5 Human 6.5 pKi = 6.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(I)cc2)CC1 10.1021/jm0200411
CHEMBL73979 202988 2 None -83 5 Human 6.5 pKi = 6.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(I)cc2)CC1 10.1021/jm0200411
10991109 203456 1 None -316 5 Human 5.5 pKi = 5.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 329 5 0 2 4.1 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/jm0200411
CHEMBL78218 203456 1 None -316 5 Human 5.5 pKi = 5.5 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 329 5 0 2 4.1 O=C(c1ccc(F)cc1)C1CCN(CCc2ccc(F)cc2)CC1 10.1021/jm0200411
155539483 172293 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL4515160 172293 0 None -42 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 504 7 2 3 5.4 O=C1CC(c2c[nH]c3ccc(F)cc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
71574302 85837 0 None -27 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312637 85837 0 None -27 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
156013612 176654 0 None -30 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 452 9 0 7 5.9 c1ccc2oc(SCCCCCCN3CCN(c4nsc5ccccc45)CC3)nc2c1 10.1016/j.bmc.2020.115459
CHEMBL4635603 176654 0 None -30 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 452 9 0 7 5.9 c1ccc2oc(SCCCCCCN3CCN(c4nsc5ccccc45)CC3)nc2c1 10.1016/j.bmc.2020.115459
138691317 170971 0 None -5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 211 2 1 2 3.1 CCn1cncc1-c1c[nH]c2ccccc12 10.1016/j.ejmech.2019.03.017
CHEMBL4464377 170971 0 None -5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 211 2 1 2 3.1 CCn1cncc1-c1c[nH]c2ccccc12 10.1016/j.ejmech.2019.03.017
168292270 191291 2 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 5 1 5 4.8 COc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5199814 191291 2 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 387 5 1 5 4.8 COc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
156010319 176468 0 None -54 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115459
CHEMBL4632519 176468 0 None -54 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 443 8 0 4 4.1 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115459
155530553 170966 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 3 4.8 Cn1cc(CCNCc2ccc(-c3ccccc3)o2)c2ccccc21 10.1016/j.ejmech.2019.111857
CHEMBL4464285 170966 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 3 4.8 Cn1cc(CCNCc2ccc(-c3ccccc3)o2)c2ccccc21 10.1016/j.ejmech.2019.111857
118464420 137717 0 None -512 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 137717 0 None -512 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
11560362 154908 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 1 1 2 4.8 CC1(c2ccc(Br)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL403843 154908 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 397 1 1 2 4.8 CC1(c2ccc(Br)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
137640705 156556 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 290 3 1 7 0.9 CN1CCN(c2nc(N)nc(Cc3cccs3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4074481 156556 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 290 3 1 7 0.9 CN1CCN(c2nc(N)nc(Cc3cccs3)n2)CC1 10.1016/j.ejmech.2017.04.033
16573 177045 30 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177045 30 None -15 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
122179556 120974 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 nan
CHEMBL3582461 120974 0 None -2 2 Human 5.5 pKi = 5.5 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000733a HTR6
ChEMBL 303 2 0 3 4.5 FC(F)(F)c1ccc2c(c1)nc(-c1cccnc1)n2C1CC1 nan
68115781 131738 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 3 2 5 2.0 NC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696973 131738 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 3 2 5 2.0 NC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
57392825 68055 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL1916744 68055 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233402 68055 0 None -234 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 496 9 0 4 4.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(c2ccccc2)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
137655411 158210 0 None -10 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4093971 158210 0 None -10 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
44388953 123172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL362177 123172 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 398 4 2 7 2.7 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3ccc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2004.10.064
16118927 59817 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1642871 59817 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
CHEMBL1739586 59817 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1)C1CCNCC1 10.1016/j.bmc.2010.10.033
16718921 182078 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 O=S(=O)(Nc1ccc2c(c1)C(CCN1CCCCC1)=CC2)c1c(Cl)nc2sccn12 10.1021/jm8009469
CHEMBL478895 182078 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 462 6 1 6 4.7 O=S(=O)(Nc1ccc2c(c1)C(CCN1CCCCC1)=CC2)c1c(Cl)nc2sccn12 10.1021/jm8009469
155562423 174653 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
CHEMBL4571469 174653 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 438 6 2 6 3.8 CCc1nc(NC(C)=O)[nH]c1-c1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.ejmech.2019.06.001
23655664 170811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 374 4 1 5 3.7 NCCc1cn(S(=O)(=O)c2cc(Cl)c(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL446194 170811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 374 4 1 5 3.7 NCCc1cn(S(=O)(=O)c2cc(Cl)c(Cl)s2)c2ccccc12 10.1021/jm070521y
24784323 176409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 377 3 1 6 2.7 O=S(=O)(c1cccc(Cl)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL462529 176409 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 377 3 1 6 2.7 O=S(=O)(c1cccc(Cl)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
155543869 174438 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4566992 174438 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
57398615 71205 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949768 71205 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963025 71205 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 373 4 1 5 3.1 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68109540 131127 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692869 131127 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 373 2 1 4 4.3 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
137661837 158677 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4098815 158677 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 421 4 0 5 3.4 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3cccc(Cl)c23)CC1 10.1021/acs.jmedchem.6b01662
11271219 129105 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 463 6 1 7 4.3 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367305 129105 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 463 6 1 7 4.3 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
58158709 138629 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787246 138629 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 347 4 2 3 2.2 CCN/C(=N\S(=O)(=O)c1ccc2cc[nH]c2c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
17940055 51020 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 417 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(F)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL158094 51020 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 417 5 2 5 2.8 COc1ccc(S(=O)(=O)Nc2cc(F)cc(F)c2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328649 205920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@@H](C)NC[C@@H]4C)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95285 205920 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@@H](C)NC[C@@H]4C)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918748 126306 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1021/jm050247c
CHEMBL365471 126306 2 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 326 2 1 4 3.3 Nc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCCC3)cc1 10.1021/jm050247c
46890263 6609 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 451 5 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2010.03.110
CHEMBL1083481 6609 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 451 5 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CNS(=O)(=O)C(F)(F)F 10.1016/j.bmcl.2010.03.110
46890292 7180 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 423 4 0 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CCCS1(=O)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1085879 7180 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 423 4 0 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)CCC[C@H]2CN1CCCS1(=O)=O 10.1016/j.bmcl.2010.03.110
44425717 85920 0 None -39 5 Human 7.5 pKi = 7.5 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 484 6 1 4 5.6 CC(C)Oc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231349 85920 0 None -39 5 Human 7.5 pKi = 7.5 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 484 6 1 4 5.6 CC(C)Oc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
164624246 185361 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4869411 185361 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
2853434 117428 14 None -2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 386 3 1 2 4.9 O=S(=O)(c1ccccc1)N1C=Cc2ccccc2C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403335 117428 14 None -2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 386 3 1 2 4.9 O=S(=O)(c1ccccc1)N1C=Cc2ccccc2C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
145985533 165179 0 None -309 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246202 165179 0 None -309 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
10202564 1496 8 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
3217 1496 8 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
CHEMBL362628 1496 8 None - 1 Human 6.5 pKi = 6.5 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 10.1016/j.ejmech.2018.11.017
145959790 161743 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.0 Cc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164195 161743 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.0 Cc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
137657317 159081 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 3 4.2 CN1CCN(Cc2cn(Cc3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103475 159081 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 3 4.2 CN1CCN(Cc2cn(Cc3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
71458647 81001 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 434 9 1 4 4.0 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159457 81001 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 434 9 1 4 4.0 CC(C)c1ccccc1OCCN1CCC(CNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.043
145984299 165199 0 None -2238 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4246655 165199 0 None -2238 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
90654856 112196 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233677 112196 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304304 112196 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2014.01.065
71449641 81002 0 None -24 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 468 9 1 4 4.6 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159458 81002 0 None -24 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 468 9 1 4 4.6 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
6484477 174308 9 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 276 2 0 5 2.3 CCc1cc2c(N3CCN(C)CC3)nc(C)nc2s1 10.1016/j.ejmech.2019.111857
CHEMBL4563932 174308 9 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 276 2 0 5 2.3 CCc1cc2c(N3CCN(C)CC3)nc(C)nc2s1 10.1016/j.ejmech.2019.111857
11397149 56181 0 None -1000 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632223 56181 0 None -1000 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
134139144 145582 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3919497 145582 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
134147644 149105 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3947289 149105 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@@H]1c2cc3c(ccn3S(=O)(=O)c3ccccc3)cc2[C@@H]1CCO 10.1016/j.bmc.2016.10.010
22557286 93077 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 1 7 1.1 CS(=O)(=O)c1ccccc1S(=O)(=O)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
CHEMBL246290 93077 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 1 7 1.1 CS(=O)(=O)c1ccccc1S(=O)(=O)N1CCOc2c(N3CCNCC3)cccc21 10.1016/j.bmcl.2006.12.093
11304596 56102 0 None -19952 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631542 56102 0 None -19952 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
10573876 10363 0 None -1584 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
CHEMBL116448 10363 0 None -1584 7 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
156016366 177065 0 None -39 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 458 10 1 6 4.0 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
CHEMBL4641296 177065 0 None -39 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 458 10 1 6 4.0 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccccc1 10.1016/j.bmc.2020.115459
145974789 162502 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 3 1 5 2.3 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176229 162502 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 325 3 1 5 2.3 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
242 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
34 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
60795 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
CHEMBL1112 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
DB01238 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2021.127909
242 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
34 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
60795 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
CHEMBL1112 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
DB01238 467 117 None -144 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2020.112709
155515408 175758 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4442062 175758 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595453 175758 0 None -15 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 491 8 0 3 5.9 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2019.06.028
16040768 113655 0 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 452 4 2 4 5.3 O=S(=O)(Nc1ccc2c(c1)CNCCC2)c1csc(C(F)(F)F)c1-c1ccccc1 10.1021/jm5003952
CHEMBL3329424 113655 0 None - 1 Human 7.5 pKi = 7.5 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 452 4 2 4 5.3 O=S(=O)(Nc1ccc2c(c1)CNCCC2)c1csc(C(F)(F)F)c1-c1ccccc1 10.1021/jm5003952
20722800 66600 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL186621 66600 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
20722800 66600 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL186621 66600 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
137657598 159076 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 352 3 1 6 2.1 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4103397 159076 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 352 3 1 6 2.1 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
57392615 70426 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 341 2 1 5 2.6 Cn1c2c(c3cc(S(=O)(=O)n4cccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950772 70426 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 341 2 1 5 2.6 Cn1c2c(c3cc(S(=O)(=O)n4cccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57396848 71192 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949760 71192 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962943 71192 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1F 10.1016/j.bmcl.2011.12.026
56944668 111620 0 None -39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3290005 111620 0 None -39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
16222762 81640 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 386 3 0 4 3.7 Cc1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165555 81640 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 386 3 0 4 3.7 Cc1ccc(S(=O)(=O)n2c3c(c4cc(F)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
16222865 81619 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165535 81619 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.bmcl.2012.06.002
11729763 118019 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 434 8 0 5 4.6 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OCc3ccccc3)cc12 10.1021/jm010943m
CHEMBL341495 118019 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 434 8 0 5 4.6 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OCc3ccccc3)cc12 10.1021/jm010943m
66800965 157649 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4087852 157649 0 None -173 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 461 8 2 3 4.8 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(F)c1 10.1021/acs.jmedchem.7b00839
145955674 161881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)nccc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4166372 161881 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)nccc32)c1 10.1016/j.ejmech.2017.12.053
56595533 65316 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
CHEMBL1834237 65316 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 391 4 1 4 2.8 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccncc1 10.1021/jm200466r
135458672 117430 10 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 3 2 3 4.1 Cc1ccc(S(=O)(=O)N/N=C2\CCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403337 117430 10 None 1 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 387 3 2 3 4.1 Cc1ccc(S(=O)(=O)N/N=C2\CCCc3c2[nH]c2ccc(Cl)cc32)cc1 10.1016/j.bmcl.2015.03.049
156017397 177123 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 420 7 1 4 5.0 CCCC(=O)Nc1ccc2c(c1)-c1c(OCC3CC3)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4642034 177123 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 420 7 1 4 5.0 CCCC(=O)Nc1ccc2c(c1)-c1c(OCC3CC3)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
168287126 190969 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 414 6 3 7 2.9 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194826 190969 0 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 414 6 3 7 2.9 Nc1nc(NCCc2c[nH]c3ccccc23)nc(N2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
44568103 183442 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 424 4 0 5 4.2 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482100 183442 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 424 4 0 5 4.2 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C2CCCC2)CC3)c1 10.1016/j.bmcl.2008.06.030
127037679 136152 0 None -40 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 438 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cc(F)ccc2F)CC1 10.1039/C5MD00166H
CHEMBL3740235 136152 0 None -40 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 438 8 1 4 3.9 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cc(F)ccc2F)CC1 10.1039/C5MD00166H
127026133 137296 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 5.4 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759819 137296 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 5.4 O=S(=O)(NC1CC2CCC(C1)N2CCOc1cccc(-c2ccccc2)c1)c1cccc(Cl)c1 10.1016/j.ejmech.2015.11.040
71574208 85842 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312642 85842 0 None -12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
137634216 156107 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 3 0 4 4.0 CN1CCN(Cc2cn(C(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4069315 156107 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 3 0 4 4.0 CN1CCN(Cc2cn(C(=O)c3ccccc3Br)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
162652175 179693 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 284 3 0 2 4.8 c1ccc(Cn2ccc3ccc(-c4ccncc4)cc32)cc1 10.1016/j.ejmech.2020.112916
CHEMBL4750657 179693 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 284 3 0 2 4.8 c1ccc(Cn2ccc3ccc(-c4ccncc4)cc32)cc1 10.1016/j.ejmech.2020.112916
71449643 81026 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159481 81026 0 None -45 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155549315 173257 0 None -1621 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 448 9 0 6 4.1 COc1ccccc1N1CCN(CCCCCCn2c(=O)n3c4c(cccc42)CCC3)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4538667 173257 0 None -1621 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 448 9 0 6 4.1 COc1ccccc1N1CCN(CCCCCCn2c(=O)n3c4c(cccc42)CCC3)CC1 10.1016/j.bmcl.2019.06.029
156020902 177455 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 378 5 0 4 4.3 COc1cc2c3c(c1OCC1CC1)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4646861 177455 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 378 5 0 4 4.3 COc1cc2c3c(c1OCC1CC1)-c1cc(N(C)C)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
44327972 205857 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1016/j.bmcl.2005.01.031
CHEMBL94969 205857 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1016/j.bmcl.2005.01.031
9863380 18158 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 353 5 0 5 2.9 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(C#N)cc12 10.1021/jm010943m
CHEMBL127089 18158 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 353 5 0 5 2.9 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(C#N)cc12 10.1021/jm010943m
44327972 205857 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1021/jm030030n
CHEMBL94969 205857 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 0 3 3.7 COc1ccc2c(c1)c(CCN(C)C)cn2-c1ccccc1 10.1021/jm030030n
100 3745 52 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -17 55 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
44568022 182423 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
CHEMBL479362 182423 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 356 3 1 5 2.6 COc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)cc1 10.1016/j.bmcl.2008.06.030
44567933 187710 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1cccc(F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL500305 187710 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 344 2 1 4 2.7 O=S(=O)(c1cccc(F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
145955822 162125 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4170187 162125 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 327 3 1 5 2.5 Clc1cccc(Cn2cnc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
616691 153821 13 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 6 2 5 2.7 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL398698 153821 13 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 6 2 5 2.7 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
44403061 126898 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 1 4 3.5 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL365993 126898 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 1 4 3.5 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44591068 189978 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518017 189978 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 411 3 1 6 3.1 O=S(=O)(c1ccc(C(F)(F)F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
5 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
5202 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
CHEMBL39 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
DB08839 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm401895u
5 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
5202 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
CHEMBL39 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
DB08839 139 66 None -169 54 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2014.12.045
118731509 117743 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 9 1 6 4.5 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409244 117743 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 515 9 1 6 4.5 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
66801173 111571 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 486 8 1 7 4.4 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289958 111571 0 None -5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 486 8 1 7 4.4 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44435632 89039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL237179 89039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44435632 89039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL237179 89039 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 403 4 0 5 4.2 CCN1CCCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
197033 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
CHEMBL589390 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]Lysergic acid from human recombinant 5HT6 receptor expressed in human HeLa cells
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2009.11.037
56595280 65305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834225 65305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595280 65305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834225 65305 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 308 4 1 3 1.7 CCN/C(=N\S(=O)(=O)c1ccccc1)N1CC(CC)C=N1 10.1021/jm200466r
56595407 65312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
CHEMBL1834231 65312 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 314 3 1 3 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CCC=N1 10.1021/jm200466r
4806 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
66803500 155898 0 None -131 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 459 8 3 4 4.4 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4066971 155898 0 None -131 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 459 8 3 4 4.4 O=S(=O)(NCCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc(O)c1 10.1021/acs.jmedchem.7b00839
54586020 62211 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782365 62211 0 None -3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
90656175 110357 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260808 110357 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 328 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNC2 10.1016/j.bmcl.2014.03.049
66801226 111585 0 None -33 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 7 1 6 3.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289971 111585 0 None -33 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 7 1 6 3.1 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
9419 35693 29 None -165 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL1442422 35693 29 None -165 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1016/j.bmcl.2020.127493
168295653 191730 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 4 1 4 5.5 Clc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5206513 191730 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 4 1 4 5.5 Clc1cccc(Cn2ccc3c(NC4CCOCC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
155543054 172616 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 358 8 1 2 5.9 CCCN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4522432 172616 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 358 8 1 2 5.9 CCCN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
11306131 60198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4c(N(C)C)cccc34)CC1)C(=O)OC2 10.1021/jm049615n
CHEMBL175718 60198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 4.5 Cc1cccc2c1N(C1CCN(S(=O)(=O)c3cccc4c(N(C)C)cccc34)CC1)C(=O)OC2 10.1021/jm049615n
145986031 165269 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248544 165269 0 None -22 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 0 6 5.2 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
126720389 161572 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 337 4 1 6 2.2 COc1ccccc1Cn1c(C)nc2c(N3CCNCC3)ccnc21 10.1016/j.ejmech.2017.12.053
CHEMBL4161480 161572 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 337 4 1 6 2.2 COc1ccccc1Cn1c(C)nc2c(N3CCNCC3)ccnc21 10.1016/j.ejmech.2017.12.053
44581974 175131 0 None -64 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 175131 0 None -64 9 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
57403839 71202 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949967 71202 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963008 71202 0 None -2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
68109250 131108 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692850 131108 0 None - 1 Human 6.5 pKi = 6.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1cc(F)cc(F)c1)c1ccc2oc3c(c2c1)CNCC3 nan
44390054 64142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 283 2 1 3 3.3 Nc1ccc(S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL181382 64142 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 283 2 1 3 3.3 Nc1ccc(S(=O)(=O)c2cccc3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
197033 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2021.128275
CHEMBL589390 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.bmcl.2021.128275
197033 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL589390 197473 58 None -3 8 Human 7.5 pKi = 7.5 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 319 3 0 3 3.9 Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1 10.1016/j.ejmech.2009.10.035
23900125 162832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 415 7 1 6 2.9 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/s0960-894x(03)00612-7
CHEMBL419398 162832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 415 7 1 6 2.9 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(NC(C)=O)cc1 10.1016/s0960-894x(03)00612-7
66800959 156896 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 413 6 2 3 3.7 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4078873 156896 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 413 6 2 3 3.7 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
90469184 185050 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4864338 185050 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 460 3 1 6 3.9 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
44403057 132902 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 4 1 4 3.8 O=S(=O)(c1ccc(I)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL370508 132902 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 466 4 1 4 3.8 O=S(=O)(c1ccc(I)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398718 69402 0 None -6 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69402 0 None -6 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
45488152 197251 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL584690 197251 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 370 3 1 4 3.7 CN1CCN(c2cccc3[nH]c(C(=O)c4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
155522117 175783 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4450907 175783 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4595675 175783 0 None 67 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 338 3 2 5 2.9 Nc1ncc(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
11383990 200095 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
CHEMBL606766 200095 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 399 6 2 4 3.6 COc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@@H]4CCCN4C)c3c2)cc1 10.1021/jm049243i
68109087 131138 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 378 2 1 5 4.0 O=S(=O)(c1ccc2c3c(oc2c1)CC1CCC3N1)n1ccc2ccccc21 nan
CHEMBL3692879 131138 0 None - 1 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 378 2 1 5 4.0 O=S(=O)(c1ccc2c3c(oc2c1)CC1CCC3N1)n1ccc2ccccc21 nan
162656718 180376 0 None -8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
CHEMBL4758402 180376 0 None -8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
137630632 160534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4097893 160534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116776 160534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 1 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(O)cc23)CC1 10.1021/acs.jmedchem.6b01662
162651101 179654 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 601 15 2 6 6.1 C[C@H](NCc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4750021 179654 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 601 15 2 6 6.1 C[C@H](NCc1ccc(OCCCCCCN2CCN(c3cccc4c3ccn4Cc3cccc(Cl)c3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
3132842 162437 9 None 10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 411 9 1 4 5.4 CCC1(C)CC(CCNCc2ccc(OC)c(OC)c2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
CHEMBL4175296 162437 9 None 10 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 411 9 1 4 5.4 CCC1(C)CC(CCNCc2ccc(OC)c(OC)c2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
58258803 127428 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)ccn4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664775 127428 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 371 2 1 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)ccn4)ccc31)C1CCC(C2)N1 nan
145983468 164884 0 None -31 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238897 164884 0 None -31 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cccc2ncccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
11609368 154720 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 2 1 3 3.4 COc1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL402810 154720 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 315 2 1 3 3.4 COc1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
134142907 144766 0 None -39 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3913100 144766 0 None -39 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 469 10 1 6 3.5 N#Cc1ccc(CNC(=O)CCOCCN2CCN(c3cccnc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155532544 171185 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.9 COc1ccc2[nH]cc(CC(C)NCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4467357 171185 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 7 3 4 4.9 COc1ccc2[nH]cc(CC(C)NCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
11501432 94274 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 2 1 3 4.2 CN(C)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL252902 94274 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 2 1 3 4.2 CN(C)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
155538144 171830 0 None -12 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 295 3 1 3 4.0 CCn1cncc1-c1c[nH]c2ccc(OC(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4476520 171830 0 None -12 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 295 3 1 3 4.0 CCn1cncc1-c1c[nH]c2ccc(OC(F)(F)F)cc12 10.1016/j.ejmech.2019.03.017
155561901 175183 0 None -75 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 259 3 1 3 3.2 CCn1cncc1-c1c[nH]c2ccc(OC)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4583507 175183 0 None -75 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 259 3 1 3 3.2 CCn1cncc1-c1c[nH]c2ccc(OC)c(F)c12 10.1016/j.ejmech.2019.03.017
155547436 173000 0 None -7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2019.06.029
CHEMBL4532741 173000 0 None -7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1cccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2019.06.029
145984511 165072 0 None -34 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243497 165072 0 None -34 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 493 6 0 7 3.8 O=S(=O)(c1cncc2ccccc12)N1CC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
137650870 156620 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 7 0 6 3.7 COc1ccc2c(c1)c(CN1CCN(CCF)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4075316 156620 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 7 0 6 3.7 COc1ccc2c(c1)c(CN1CCN(CCF)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137661730 158958 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 478 5 0 7 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)nn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4101944 158958 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 478 5 0 7 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)nn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
142601325 185287 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4868035 185287 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.9 c1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
58258800 127389 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 4 3.9 [C-]#[N+]c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664735 127389 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 4 3.9 [C-]#[N+]c1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
44390023 11642 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1181573 11642 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL180945 11642 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 302 3 1 2 3.8 c1ccc(Cc2ccc(N3CCNCC3)c3ccccc23)cc1 10.1016/j.bmcl.2005.01.031
191 399 92 None -20 28 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -20 28 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -20 28 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -20 28 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -20 28 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
56945042 157497 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4085802 157497 0 None -3 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b00839
52913226 70421 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C#N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950766 70421 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C#N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
45487150 196043 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL571413 196043 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 335 4 1 5 2.5 NCCn1cc(S(=O)(=O)c2cccc(Cl)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
90644077 111595 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 7 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289981 111595 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 7 3.5 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
66801028 111611 0 None -9 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 8 1 6 4.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289997 111611 0 None -9 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 501 8 1 6 4.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
11407544 200522 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 421 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3Cl)cc12 10.1021/jm049243i
CHEMBL609736 200522 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 421 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(F)cc3Cl)cc12 10.1021/jm049243i
58149665 81932 2 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172183 81932 2 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
137650795 156901 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4078912 156901 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
58149672 81933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 392 3 0 7 2.4 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccc(F)cc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172184 81933 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 392 3 0 7 2.4 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccc(F)cc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
57392612 70410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
58258855 127425 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 414 3 1 4 4.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2-c2ccccc2)CC2CCC1N2 nan
CHEMBL3664771 127425 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 414 3 1 4 4.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2-c2ccccc2)CC2CCC1N2 nan
10111488 17814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 398 6 0 5 3.9 COc1ccc2c(c1)c(CCN1CCCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126263 17814 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 398 6 0 5 3.9 COc1ccc2c(c1)c(CCN1CCCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
66801625 157740 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 7 2 3 5.7 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
CHEMBL4088925 157740 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 493 7 2 3 5.7 Cc1[nH]c2ccc(Cl)cc2c1C1=CCN(CCCNS(=O)(=O)c2ccc3ccccc3c2)CC1 10.1021/acs.jmedchem.7b00839
168280347 190575 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
CHEMBL5188859 190575 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)C1 10.1016/j.ejmech.2022.114329
57392612 70410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950755 70410 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL5081379 212974 0 None -524 9 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
156013736 176689 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 404 6 1 4 4.2 C#CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4636165 176689 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 404 6 1 4 4.2 C#CCOc1c(OC)cc2c3c1-c1cc(NC(=O)CCC)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
90666903 108961 0 None -44 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
CHEMBL3220219 108961 0 None -44 7 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
164608896 183838 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4846146 183838 0 None 5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155544139 172781 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(OCc2nc(N)nc(N3CCN(C)CC3)n2)ccc1Cl 10.1016/j.ejmech.2019.06.022
CHEMBL4527124 172781 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(OCc2nc(N)nc(N3CCN(C)CC3)n2)ccc1Cl 10.1016/j.ejmech.2019.06.022
156022234 177636 0 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 380 5 1 4 4.2 CCCC(=O)Nc1ccc2c(c1)-c1c(OC)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
CHEMBL4649697 177636 0 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 380 5 1 4 4.2 CCCC(=O)Nc1ccc2c(c1)-c1c(OC)c(OC)cc3c1C(C2)N(C)CC3 10.1016/j.bmc.2020.115578
57384073 76852 0 None -4466 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 COc1ccccc1N1CCN(CCCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL2079256 76852 0 None -4466 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 COc1ccccc1N1CCN(CCCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
71458652 81023 0 None -35 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159478 81023 0 None -35 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 410 8 1 5 3.0 CSc1ccccc1OCCN1CCC(NS(=O)(=O)c2ccc(F)cc2)C1 10.1016/j.ejmech.2012.07.043
155515324 169388 0 None 3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 382 4 1 8 0.8 CN1CCN(c2nc(N)nc(CS(=O)(=O)c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4441655 169388 0 None 3 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 382 4 1 8 0.8 CN1CCN(c2nc(N)nc(CS(=O)(=O)c3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.06.022
3649661 137691 6 None -489 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 137691 6 None -489 8 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
26987 936 29 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -58 21 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
137641832 157698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 327 3 1 5 2.6 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
CHEMBL4088416 157698 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 327 3 1 5 2.6 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
137651887 156757 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 7 2 3 4.6 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4077040 156757 0 None -7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 443 7 2 3 4.6 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
145953749 161838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 4 1 5 2.5 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4165620 161838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 321 4 1 5 2.5 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
134131482 141600 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 649 13 1 7 7.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3883432 141600 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 649 13 1 7 7.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134131347 141707 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 635 12 1 7 7.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884690 141707 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 635 12 1 7 7.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
127046963 139044 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 413 5 0 7 2.7 CC(C)CS(=O)(=O)n1ccc2c(-c3cccnc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797293 139044 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 413 5 0 7 2.7 CC(C)CS(=O)(=O)n1ccc2c(-c3cccnc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
24784577 189768 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 5 0 6 4.3 CCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL517707 189768 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 435 5 0 6 4.3 CCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
11338273 200111 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
CHEMBL606868 200111 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1cccc(Cl)c1 10.1021/jm049243i
137634321 155822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(C(C)C)cc3)c2c1 10.1021/acs.jmedchem.6b01662
CHEMBL4066047 155822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 441 6 0 6 3.8 COc1ccc2c(CN3CCN(C)CC3)cn(S(=O)(=O)c3ccc(C(C)C)cc3)c2c1 10.1021/acs.jmedchem.6b01662
45488165 195236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
CHEMBL566218 195236 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 356 3 1 3 4.1 CN1CCN(c2cccc3[nH]c(Cc4cccc5ccccc45)nc23)CC1 10.1021/jm901672k
69485025 155484 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 505 6 0 6 4.2 CC(C)Oc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4062233 155484 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 505 6 0 6 4.2 CC(C)Oc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
25117681 198872 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
CHEMBL599023 198872 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CC[C@@H](N)C3)ccc21 10.1021/jm901674f
66801701 158782 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 471 8 2 3 5.3 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4099997 158782 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 471 8 2 3 5.3 Cc1cccc(S(=O)(=O)NCCCCN2CC=C(c3c(C)[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
162653506 179950 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCCCC3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4753614 179950 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCCCC3)ccc21 10.1016/j.ejmech.2020.112916
145984737 165027 0 None -724 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242392 165027 0 None -724 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
135367816 164283 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218801 164283 0 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 248 1 1 3 2.7 Clc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
173 3211 88 None -41 22 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
5011 3211 88 None -41 22 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
CHEMBL18772 3211 88 None -41 22 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm030030n
57392612 70410 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950755 70410 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 3 1 4 4.4 CC(C)n1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
68639205 160420 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4099525 160420 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4115947 160420 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 537 5 0 5 4.6 O=C(c1ccccc1)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
145962993 160879 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4126962 160879 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
155516282 169502 0 None -20 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)cc1 10.1016/j.bmcl.2019.06.029
CHEMBL4443185 169502 0 None -20 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 443 9 0 4 5.2 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc3c45)CC2)cc1 10.1016/j.bmcl.2019.06.029
22028199 196658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL576312 196658 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 329 5 0 5 2.4 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ncccc21 10.1016/j.bmcl.2009.10.067
164616980 184700 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 8 1 5 5.3 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4859019 184700 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 463 8 1 5 5.3 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3Cc2ccccc2)C1 10.1016/j.ejmech.2021.113792
57401298 70416 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950761 70416 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 nan
58258819 127395 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5ccccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664741 127395 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 402 2 1 4 4.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc5ccccc5c4)ccc31)C1CCC(C2)N1 nan
44414681 79780 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1ccc(S(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
CHEMBL213589 79780 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1ccc(S(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
155527391 170675 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
CHEMBL4459863 170675 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cnc2ccccc2c1)n1cc(C2=CCNCC2)c2ccc(Cl)cc21 10.1021/acsmedchemlett.6b00056
162647987 179334 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 437 4 1 7 2.9 O=S(=O)(c1cccc(F)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
CHEMBL4746063 179334 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 437 4 1 7 2.9 O=S(=O)(c1cccc(F)c1)n1c(-c2ccccc2)nc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.0c02009
57401298 70416 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950761 70416 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccc(Cl)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
57403833 71126 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949765 71126 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962396 71126 0 None 6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68115688 131192 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 2 1 6 3.5 Cn1ncc2cc(S(=O)(=O)c3cc(Cl)c4oc5c(c4c3)CNCC5)ccc21 nan
CHEMBL3692933 131192 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 2 1 6 3.5 Cn1ncc2cc(S(=O)(=O)c3cc(Cl)c4oc5c(c4c3)CNCC5)ccc21 nan
162674561 182689 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
CHEMBL4796647 182689 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 403 7 1 5 3.0 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112149
137648438 157337 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 483 6 0 7 3.5 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4083959 157337 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 483 6 0 7 3.5 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(OC(F)(F)F)cc1 10.1021/acs.jmedchem.6b01662
9817950 17844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 304 3 1 5 3.2 CN(C)CCc1cn(C(=O)OC(C)(C)C)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL126420 17844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 304 3 1 5 3.2 CN(C)CCc1cn(C(=O)OC(C)(C)C)c2ccc(O)cc12 10.1021/jm010943m
2921525 54585 13 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL1379600 54585 13 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL1613157 54585 13 None 3 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 375 8 1 4 4.7 COc1ccc(CNCCC(c2ccccc2)c2ccc3c(c2)OCO3)cc1 10.1016/j.ejmech.2018.04.010
44476801 81937 2 None - 1 Human 6.4 pKi = 6.4 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
CHEMBL2172189 81937 2 None - 1 Human 6.4 pKi = 6.4 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 nan
44476801 81937 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
CHEMBL2172189 81937 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCN(C)C3 10.1016/j.bmcl.2012.05.036
117209964 185552 1 None -5 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4871980 185552 1 None -5 4 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118648 75968 0 None -74 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 75968 0 None -74 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
145971739 162544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)nccc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
CHEMBL4176992 162544 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 307 3 1 5 2.2 Cc1nc2c(N3CCNCC3)nccc2n1Cc1ccccc1 10.1016/j.ejmech.2017.12.053
155519516 175784 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4447659 175784 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595677 175784 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmc.2019.06.028
118731356 117689 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409039 117689 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 502 8 0 4 4.6 O=C([C@@H]1CCCN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1)N1CCCCC1 10.1016/j.ejmech.2014.12.041
57395086 71209 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
CHEMBL1949966 71209 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
CHEMBL1963029 71209 0 None -151 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cccc2cccnc12 10.1016/j.bmc.2011.12.039
71451456 81008 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 8 1 4 3.5 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(F)c2)CC1 10.1016/j.ejmech.2012.07.043
CHEMBL2159463 81008 0 None -50 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 8 1 4 3.5 CCOc1ccccc1C(=O)NC1CCN(CCOc2cccc(F)c2)CC1 10.1016/j.ejmech.2012.07.043
156016485 177199 0 None -380 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 0 7 4.7 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2cccc3c2n1CCC3 10.1016/j.bmc.2020.115459
CHEMBL4642981 177199 0 None -380 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 0 7 4.7 O=c1n(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2cccc3c2n1CCC3 10.1016/j.bmc.2020.115459
11849203 79446 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.2 CNCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212227 79446 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 290 6 2 3 2.2 CNCCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
15281645 167785 7 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
CHEMBL434365 167785 7 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/jm060469q
162673219 182562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4795207 182562 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
118626161 165047 0 None -53 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4242858 165047 0 None -53 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
162647425 178997 0 None 10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4741978 178997 0 None 10 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 584 13 0 7 5.3 C#CCN(C)Cc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
15281645 167785 7 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.7b00085
CHEMBL434365 167785 7 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.7b00085
57402070 71219 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949761 71219 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1963096 71219 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1ccccc1Cl 10.1016/j.bmcl.2011.12.026
68109060 131103 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccc(Cl)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692845 131103 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1ccc(Cl)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
68109319 131106 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692848 131106 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.2 Cc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
162659287 180707 0 None -34 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4762226 180707 0 None -34 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
162666577 181751 0 None -28 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4784414 181751 0 None -28 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 455 7 1 6 4.3 Cc1ccc2sc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cc2c1 10.1016/j.ejmech.2020.112149
53327611 69411 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
162647097 179139 0 None -41 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4744007 179139 0 None -41 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
44393113 63300 0 None -190 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 358 7 3 7 3.5 CC(Nc1nc(N)nc(NCCc2cccs2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
CHEMBL180086 63300 0 None -190 3 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-Hydroxy tryptamine 6 receptorBinding affinity against 5-Hydroxy tryptamine 6 receptor
ChEMBL 358 7 3 7 3.5 CC(Nc1nc(N)nc(NCCc2cccs2)n1)c1ccc(F)cc1 10.1016/j.bmcl.2004.06.008
155557443 174072 0 None -181 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 3 2.7 COc1ccc2[nH]cc(-c3cncn3C)c2c1F 10.1016/j.ejmech.2019.03.017
CHEMBL4558202 174072 0 None -181 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 3 2.7 COc1ccc2[nH]cc(-c3cncn3C)c2c1F 10.1016/j.ejmech.2019.03.017
137637994 155401 0 None -26 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4061131 155401 0 None -26 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cncc2ccccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
164614828 184687 0 None 3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4858771 184687 0 None 3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
168290376 191348 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 411 3 0 3 6.1 FC1(F)CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5200705 191348 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 411 3 0 3 6.1 FC1(F)CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
44582675 189109 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189109 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
137633663 156061 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 4 0 5 3.3 CC(=O)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4068846 156061 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 475 4 0 5 3.3 CC(=O)N1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
57400277 71217 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949771 71217 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963078 71217 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1ccc(F)cc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
168287508 190935 0 None -97 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 438 9 3 8 3.1 Nc1nc(N)nc(NCCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5194270 190935 0 None -97 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 438 9 3 8 3.1 Nc1nc(N)nc(NCCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.ejmech.2021.113931
164613499 184455 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 358 8 1 3 4.4 c1ccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4855189 184455 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 358 8 1 3 4.4 c1ccc(CNCCOc2cccc3c2CCN3Cc2ccccc2)cc1 10.1016/j.ejmech.2021.113792
44455426 154610 0 None -54 12 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 154610 0 None -54 12 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned 5HT6 receptor by competitive binding experimentInhibition of human cloned 5HT6 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
58258854 128449 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4ccnc5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3669648 128449 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 403 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)c4ccnc5ccccc45)ccc31)C1CCC(C2)N1 nan
134131296 141624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 557 9 1 7 4.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3883620 141624 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 557 9 1 7 4.3 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCNC4CCN(Cc5ccccc5)CC4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
71458723 83996 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2163740 83996 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219873 83996 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 424 3 1 5 3.7 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc(C(F)(F)F)c2)CCC(N)C1 10.1016/j.bmcl.2012.06.002
25263323 184463 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485531 184463 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 4 1 2 5.3 Cc1c(O[C@H](C)c2cccc(Cl)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25263321 184109 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL485010 184109 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
44398555 67693 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 293 4 3 5 1.7 COc1cc(N)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm050247c
CHEMBL191415 67693 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 293 4 3 5 1.7 COc1cc(N)cc(NS(=O)(=O)c2ccc(N)cc2)c1 10.1021/jm050247c
132495282 145244 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3916787 145244 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 370 5 1 5 3.0 CN(C)[C@H]1c2cc3ccn(S(=O)(=O)c4ccccc4)c3cc2[C@H]1CCO 10.1016/j.bmc.2016.10.010
46890188 7175 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 1 3 3.1 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)C(N)=O 10.1016/j.bmcl.2010.03.110
CHEMBL1085852 7175 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 376 4 1 3 3.1 CN(C[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)C(N)=O 10.1016/j.bmcl.2010.03.110
22557219 93280 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 Cc1cc(N2CC(C)NC(C)C2)c2c(c1)N(S(=O)(=O)c1ccc(Cl)cc1)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL247120 93280 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 435 3 1 5 3.4 Cc1cc(N2CC(C)NC(C)C2)c2c(c1)N(S(=O)(=O)c1ccc(Cl)cc1)CCO2 10.1016/j.bmcl.2006.12.093
162653427 179814 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 307 3 0 4 2.3 CN(C)c1cccc2c1ccn2S(=O)(=O)N1CCCCC1 10.1016/j.ejmech.2020.112916
CHEMBL4751913 179814 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 307 3 0 4 2.3 CN(C)c1cccc2c1ccn2S(=O)(=O)N1CCCCC1 10.1016/j.ejmech.2020.112916
145983018 164965 0 None -436 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
CHEMBL4240910 164965 0 None -436 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 1 7 3.0 O=c1[nH]c2c(N3CCN(CC[C@@H]4CCCN4S(=O)(=O)c4cccc5ncccc45)CC3)cccc2o1 10.1016/j.ejmech.2018.01.002
134151729 152911 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3979307 152911 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
90654854 112186 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233676 112186 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304183 112186 0 None -12 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 584 9 0 4 6.8 CC1(C)C(=O)N(Cc2ccc(Cl)cc2Cl)C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.ejmech.2014.01.065
57400281 71208 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949965 71208 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963028 71208 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccc2ncccc2c1 10.1016/j.bmc.2011.12.039
69363431 160487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4082073 160487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116440 160487 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 539 5 0 5 4.2 CN1CCN(CCc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(Br)cc23)CC1 10.1021/acs.jmedchem.6b01662
9888211 21216 9 None -501 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 21216 9 None -501 10 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11168182 3478 18 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3478 18 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3478 18 None -630 13 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 6 expressed in HeLa cells using the radioligand [3H]LSD
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
58158673 138496 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 4 2 4 1.6 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)NCC2)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785853 138496 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 4 2 4 1.6 CCN/C(=N\S(=O)(=O)c1ccc2c(c1)NCC2)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
46880532 6223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1021/jm5003952
CHEMBL1081794 6223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1021/jm5003952
11532574 113676 10 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1021/jm5003952
CHEMBL3329445 113676 10 None - 1 Human 8.4 pKi = 8.4 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1021/jm5003952
44389099 64506 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182000 64506 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 406 3 1 4 4.5 O=S(=O)(c1cccc2ccccc12)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1016/j.bmcl.2004.10.064
9927441 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL93868 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
23501288 192441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5205533 192441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL5222932 192441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 362 6 0 5 3.0 CN(C)CCOc1cccc2c1ccn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
2726 906 64 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
621 906 64 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
83 906 64 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
CHEMBL71 906 64 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
DB00477 906 64 None -10 72 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030030n
135398737 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
11532574 113676 10 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of LSD from recombinant human 5-HT6R assessed as inhibition constantDisplacement of LSD from recombinant human 5-HT6R assessed as inhibition constant
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1016/j.bmcl.2021.128275
CHEMBL3329445 113676 10 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of LSD from recombinant human 5-HT6R assessed as inhibition constantDisplacement of LSD from recombinant human 5-HT6R assessed as inhibition constant
ChEMBL 453 7 2 7 3.3 COc1cc(Cl)cc(C(C)Nc2cc(N3CCNCC3)ccc2S(C)(=O)=O)c1OC 10.1016/j.bmcl.2021.128275
137633827 156062 0 None 1071 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 377 3 1 5 3.8 O=S(=O)(c1cccc2ccccc12)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
CHEMBL4068850 156062 0 None 1071 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 377 3 1 5 3.8 O=S(=O)(c1cccc2ccccc12)n1cc2c3c(cccc31)OC(CO)=C2 10.1021/acsmedchemlett.6b00482
135398737 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
38 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
722 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
CHEMBL42 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
DB00363 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.07.043
155514378 169283 0 None 75 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cccc2ncccc12 10.1021/acsmedchemlett.6b00056
CHEMBL4440130 169283 0 None 75 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cccc2ncccc12 10.1021/acsmedchemlett.6b00056
135398737 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
38 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
722 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
CHEMBL42 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
DB00363 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2020.115578
53322547 56391 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
CHEMBL1642416 56391 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
135398737 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
38 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
722 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
CHEMBL42 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
DB00363 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2018.01.002
90469117 184323 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1cc(F)ccc1F)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4853195 184323 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 428 3 1 6 3.1 O=S(=O)(c1cc(F)ccc1F)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
134131307 141641 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 10 0 6 4.9 CN(CCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
CHEMBL3883921 141641 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 10 0 6 4.9 CN(CCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2016.08.016
137630453 160516 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4093699 160516 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116631 160516 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 5 0 5 3.9 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(F)ccc32)cc1 10.1021/acs.jmedchem.6b01662
44403092 70290 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL195018 70290 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403084 71400 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196622 71400 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 438 4 0 5 4.3 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403044 161162 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL413525 161162 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 394 4 0 5 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1016/j.bmcl.2005.07.028
46880532 6223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081794 6223 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 1 4 3.7 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
164612125 184073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.1 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4849702 184073 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 474 8 1 5 5.1 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(C(F)(F)F)c3)cccc21 10.1016/j.ejmech.2021.113792
135398737 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
38 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
722 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
CHEMBL42 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
DB00363 944 89 None -4 91 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.05.062
155535879 176095 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4472629 176095 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4598209 176095 0 None 177 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 352 3 2 5 3.2 Cc1nc(N)[nH]c1-c1ccc2ccn(S(=O)(=O)c3ccccc3)c2c1 10.1016/j.ejmech.2019.06.001
127046982 139110 0 None 93 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797717 139110 0 None 93 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
49836615 18601 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
CHEMBL1278091 18601 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4Cl)c3c2)CC1 10.1021/jm1007825
44591592 183554 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL482757 183554 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)[C@@H]1CCCNC1 10.1016/j.bmcl.2009.03.071
57396813 71201 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None 5 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
10205655 60227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL175884 60227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 473 6 2 4 5.8 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CCN4CCCC4)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
11383202 200076 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1 10.1021/jm049243i
CHEMBL606703 200076 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1 10.1021/jm049243i
11210467 200523 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
CHEMBL609737 200523 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 5 3 3 3.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1 10.1021/jm049243i
11406161 200524 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1F 10.1021/jm049243i
CHEMBL609738 200524 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 373 5 3 3 3.4 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1F 10.1021/jm049243i
11245641 200526 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 3 3 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
CHEMBL609740 200526 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 369 5 3 3 3.6 Cc1ccc(S(=O)(=O)Nc2ccc3[nH]cc(C[C@H]4CCCN4)c3c2)cc1 10.1021/jm049243i
11452988 200554 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
CHEMBL609991 200554 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 423 5 3 3 4.3 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1cccc(C(F)(F)F)c1 10.1021/jm049243i
68109120 131157 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 4 4.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CF)NCC3 nan
CHEMBL3692898 131157 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 4 4.1 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)C(CF)NCC3 nan
68115669 131195 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1ccc(F)c(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692936 131195 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1ccc(F)c(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58258848 127407 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4cc(Cl)c5ccccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664753 127407 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4cc(Cl)c5ccccc54)ccc31)C1CCC(C2)N1 nan
9927441 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
9927441 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
CHEMBL93868 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL93868 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm030030n
9927441 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL93868 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
56593798 65357 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834342 65357 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 348 4 1 4 2.4 CCN/C(=N\S(=O)(=O)c1ccc(Cl)s1)N1CC(CC)C=N1 10.1021/jm200466r
52913102 70412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950757 70412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
9927441 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL93868 205662 0 None 6 9 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm070910s
56944383 111627 0 None -9 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 111627 0 None -9 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
4106 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
5358812 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
89 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
CHEMBL93240 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2014.12.045
44474797 13950 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL1197505 13950 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
CHEMBL574625 13950 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 437 4 3 7 2.0 CN(c1ccc2c(c1)/C(=N/NC(=N)N)CC2)S(=O)(=O)c1c(Cl)nc2sccn12 10.1021/jm900796p
4106 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
5358812 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
89 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
CHEMBL93240 2466 16 None -1 33 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm401895u
25024731 62639 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 505 4 0 5 5.0 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 10.1021/ml100101u
CHEMBL1785072 62639 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 505 4 0 5 5.0 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 10.1021/ml100101u
44435620 148462 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL394231 148462 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162649235 179494 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
CHEMBL4747978 179494 0 None -6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 473 7 1 6 4.5 Cc1c(S(=O)(=O)N[C@@H]2CCN(CCCc3noc4ccccc34)C2)sc2ccc(F)cc12 10.1016/j.ejmech.2020.112149
52913102 70412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950757 70412 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(F)c4)ccc31)C1CCC(C2)N1 nan
16116899 59784 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642846 59784 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739232 59784 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NC3CCCNC3)c12 10.1016/j.bmc.2010.10.033
44435620 148462 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394231 148462 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 0 5 3.4 CN1CCC(n2cc(S(=O)(=O)c3ccc(Cl)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
45484381 196812 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
CHEMBL577687 196812 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN 10.1016/j.bmc.2009.05.055
68115746 131726 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 5 2.8 N#Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696961 131726 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 338 2 1 5 2.8 N#Cc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
16222545 81622 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165538 81622 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
44435612 88368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236405 88368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
25122651 198565 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL597002 198565 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 2 5 3.5 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)CC1 10.1021/jm901674f
58258811 127437 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127437 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
16070169 59779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642850 59779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739214 59779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 408 6 3 5 3.9 CC(C)[C@H](N)CNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
131999484 182021 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4746584 182021 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
CHEMBL4788250 182021 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 284 5 3 2 3.3 Oc1cccc(CNCCc2c[nH]c3cc(F)ccc23)c1 10.1016/j.ejmech.2020.113059
10023874 158816 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.6b01662
CHEMBL4100411 158816 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 399 5 0 6 2.6 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/acs.jmedchem.6b01662
44435612 88368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236405 88368 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 405 3 1 5 3.2 O=S(=O)(c1ccc(Br)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
71455149 81633 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Br)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165548 81633 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 462 4 0 5 4.1 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Br)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
45484398 195192 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL565977 195192 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2cc(Cl)cc(Cl)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
25263340 183588 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 368 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(F)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
CHEMBL482990 183588 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 368 4 1 3 4.7 Cc1c(C2CCNCC2)ccnc1OC(c1cccc(F)c1)C(F)(F)F 10.1016/j.bmcl.2009.03.077
10112811 165747 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
CHEMBL427134 165747 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1ccc2ccccc2c1 10.1021/jm049615n
68109102 131144 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692885 131144 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 356 2 1 5 2.9 N#Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(oc12)CCNC3 nan
68109495 131150 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CCO)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692891 131150 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 4 2 5 2.4 O=S(=O)(c1ccccc1)c1cc(CCO)c2oc3c(c2c1)CNCC3 nan
44435642 88209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL235734 88209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
58258759 127445 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 5 4.9 CC(C)n1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664792 127445 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 5 4.9 CC(C)n1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
44435642 88209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL235734 88209 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 387 4 0 5 3.7 CCN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
53327611 69411 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
68115612 131178 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cccc(CO)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692919 131178 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cccc(CO)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
25067564 199615 0 None 61 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 199615 0 None 61 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
52913108 70417 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950762 70417 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(C(F)(F)F)c4)ccc31)C1CCC(C2)N1 nan
58258862 127430 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cc[nH]c45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664777 127430 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4cccc5cc[nH]c45)ccc31)C1CCC(C2)N1 nan
16112801 180509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
CHEMBL476006 180509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1016/j.bmc.2009.08.006
137628805 160441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4077537 160441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4116136 160441 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
16112801 180509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
CHEMBL476006 180509 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 436 6 1 6 4.1 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 10.1021/jm8009469
10159058 129661 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
CHEMBL367867 129661 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 6 2 3 4.8 O=S(=O)(Nc1ccc2[nH]cc(CCN3CCCC3)c2c1)c1cccc2ccccc12 10.1021/jm049615n
68115740 131740 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cc[nH]n2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696975 131740 0 None - 1 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 2 5 3.3 O=S(=O)(c1ccccc1)c1cc(-c2cc[nH]n2)c2oc3c(c2c1)CNCC3 nan
25122653 198843 0 None 17 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
CHEMBL598850 198843 0 None 17 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 440 3 2 5 4.1 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5c(Cl)cccc45)c3c2)CC1 10.1021/jm901674f
16222870 81612 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 400 4 0 5 4.0 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165528 81612 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 400 4 0 5 4.0 CSc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435635 88772 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236772 88772 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
57399549 70411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 nan
CHEMBL1950756 70411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 nan
58258853 128476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3669675 128476 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 425 2 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cc(Cl)ccc54)ccc31)C1CCC(C2)N1 nan
44403055 69504 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193824 69504 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 338 3 1 4 3.3 O=S(=O)(c1ccccc1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435635 88772 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236772 88772 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 3.8 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
46880709 7366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
CHEMBL1086720 7366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 4 1 5 3.7 COc1ccc2c(S(=O)(=O)c3cccc(Cl)c3)cn(C3CCNC3)c2c1 10.1016/j.bmcl.2010.01.073
57399549 70411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950756 70411 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4F)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
44554393 18361 0 None 61 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1275630 18361 0 None 61 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 448 5 1 6 4.1 CC(C)Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
49836823 18523 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
CHEMBL1277466 18523 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 406 3 1 5 3.3 CN1CCN(c2cccc3c(S(=O)(=O)c4cccc5ccccc45)n[nH]c23)CC1 10.1021/jm1007825
155548127 173203 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 2.9 CCCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4537294 173203 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 2.9 CCCN1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
44435641 147064 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL393106 147064 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5084167 213127 0 None -19 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.1c00497
162647173 179051 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
CHEMBL4742856 179051 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
162643494 181067 0 None -3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4775997 181067 0 None -3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
71458812 81635 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Cl)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165550 81635 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 418 4 0 5 4.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2Cl)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
58258811 127437 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664784 127437 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5cccnc54)ccc31)C1CCC(C2)N1 nan
58258753 128482 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669681 128482 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 400 3 1 5 3.5 COc1cc(S(=O)(=O)c2ccccc2F)cc2c3c(n(C)c12)CC1CCC3N1 nan
44435641 147064 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL393106 147064 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 3 0 5 3.3 CN1CCCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
46880608 5943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080316 5943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 344 3 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
44292800 176123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 446 3 1 5 4.5 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3(O)CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45987 176123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 446 3 1 5 4.5 O=S(=O)(c1cccc2ccccc12)n1ccc2ccc(C3(O)CCN4CCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
45484382 195142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
CHEMBL565730 195142 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 343 5 0 5 2.7 Cc1c(S(=O)(=O)c2ccccc2)c2cccnc2n1CCN(C)C 10.1016/j.bmc.2009.05.055
45484297 195620 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568672 195620 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2cccnc21 10.1016/j.bmc.2009.05.055
10112809 122624 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 4 2 3 4.9 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1021/jm049615n
CHEMBL361230 122624 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 419 4 2 3 4.9 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5ccccc45)cc23)CC1 10.1021/jm049615n
57392613 70414 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 nan
CHEMBL1950759 70414 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 nan
52913100 127385 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 1 5 3.4 CN(C)Cc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
CHEMBL3664731 127385 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 4 1 5 3.4 CN(C)Cc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
58258836 127421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664767 127421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258857 128460 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
CHEMBL3669659 128460 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 2 5 3.1 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(O)c31)C1CCC(C2)N1 nan
135398737 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
38 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
722 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
CHEMBL42 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
DB00363 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00453-4
10337743 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
8429 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
CHEMBL571858 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting methodDisplacement of [3H] LSD from 5-HT6R in human HeLa cells assessed as inhibition constant incubated for 120 mins in presence of methiothepin by scintillation counting method
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2021.128275
53323439 59841 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1642873 59841 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
CHEMBL1739699 59841 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12 10.1016/j.bmc.2010.10.033
54752954 138421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785100 138421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 373 3 2 3 2.7 CCN/C(=N\S(=O)(=O)c1ccc2[nH]ccc2c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
57392613 70414 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950759 70414 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 386 2 1 4 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4Cl)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
164610173 184415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 412 8 1 5 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCCC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4854460 184415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 412 8 1 5 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCCC3)cccc21 10.1016/j.ejmech.2021.113792
10337743 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
8429 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
CHEMBL571858 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmc.2009.05.055
155542160 172544 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4520580 172544 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 397 4 0 4 3.1 O=S(=O)(c1ccccc1)N1Cc2cccc(N3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
10337743 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
8429 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
CHEMBL571858 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells by scintillation counter
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1021/acs.jmedchem.5b00179
24967099 83622 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207387 83622 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 419 4 0 5 3.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
44435627 88072 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL235070 88072 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
58258768 127415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 2 2 5 3.3 Cc1cc(S(=O)(=O)c2ccc(N)cc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664761 127415 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 2 2 5 3.3 Cc1cc(S(=O)(=O)c2ccc(N)cc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
58258772 127422 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664768 127422 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 396 4 1 5 3.8 CCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44435627 88072 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL235070 88072 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 341 3 1 5 2.8 O=S(=O)(c1ccccc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
9866222 101257 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 409 3 0 5 3.9 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
CHEMBL299569 101257 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 409 3 0 5 3.9 Cc1ccc(S(=O)(=O)n2ccc3ccc(N4CCN5CCCCC5C4)cc32)cc1 10.1016/s0960-894x(00)00320-6
10337743 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
8429 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
CHEMBL571858 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 10.1016/j.bmcl.2009.10.067
49836621 18468 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
CHEMBL1276926 18468 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 370 3 1 5 2.5 Cc1ccc(S(=O)(=O)c2n[nH]c3ccc(N4CCN(C)CC4)cc23)cc1 10.1021/jm1007825
68108527 131166 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 293 3 1 3 3.7 COc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692907 131166 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 293 3 1 3 3.7 COc1cc(Cc2ccccc2)cc2c3c(oc12)CCNC3 nan
57414528 131180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1ccc(OC(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692921 131180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 431 3 1 5 4.5 O=S(=O)(c1ccc(OC(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
10131565 116601 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 330 5 1 5 2.4 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL339337 116601 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 330 5 1 5 2.4 COc1ccc2c(c1)c(CCN)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
135 2496 38 None -21 57 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -21 57 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -21 57 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -21 57 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -21 57 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
145983961 164873 0 None -44 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238679 164873 0 None -44 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
145985692 164892 0 None -131 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239091 164892 0 None -131 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 507 6 0 7 4.2 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
44403062 71649 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 5 1 5 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL197397 71649 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 370 5 1 5 3.2 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
57393363 71220 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949764 71220 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963097 71220 0 None -3 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 349 2 1 4 3.0 O=S(=O)(c1cccc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
66800939 111566 0 None -26 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289953 111566 0 None -26 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 466 7 1 6 3.9 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
66801062 111626 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290011 111626 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 473 7 1 6 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
68109432 131107 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 328 2 2 5 2.5 Nc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692849 131107 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 328 2 2 5 2.5 Nc1ccc(S(=O)(=O)c2ccc3oc4c(c3c2)CNCC4)cc1 nan
10202396 60158 3 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL175471 60158 3 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL5077293 212720 0 None -141 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
1574 81 52 None 1 20 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
218 81 52 None 1 20 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
CHEMBL266591 81 52 None 1 20 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
22857296 28937 0 None -61 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 28937 0 None -61 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
9856041 23910 2 None -109 8 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
CHEMBL133868 23910 2 None -109 8 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligandInhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand
ChEMBL 230 2 2 2 2.4 CC(N)Cc1c[nH]c2ccc3c(c12)CCCO3 10.1021/jm030205t
11849201 77681 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccccc1N1CCNCC1 10.1021/jm060469q
CHEMBL209893 77681 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccccc1N1CCNCC1 10.1021/jm060469q
132503215 157208 0 None -10 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4082456 157208 0 None -10 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1 10.1016/j.bmc.2017.04.046
44443506 93632 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 7 1 5 4.2 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL248994 93632 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 377 7 1 5 4.2 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
162657904 180531 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCCCC3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4760297 180531 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 340 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCCCC3)cc21 10.1016/j.ejmech.2020.112916
168278234 190487 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 365 5 1 4 4.3 CN(CCO)c1nc2ccccc2c2c1ccn2Cc1cccc(Cl)c1 10.1016/j.ejmech.2022.114329
CHEMBL5187539 190487 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 365 5 1 4 4.3 CN(CCO)c1nc2ccccc2c2c1ccn2Cc1cccc(Cl)c1 10.1016/j.ejmech.2022.114329
6758 166563 73 None - 1 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
CHEMBL429023 166563 73 None - 1 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 394 3 0 6 3.7 C=C(C)[C@H]1Cc2c(ccc3c2O[C@@H]2COc4cc(OC)c(OC)cc4[C@@H]2C3=O)O1 nan
168288780 190852 0 None -23 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5193103 190852 0 None -23 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 447 8 0 6 3.9 O=c1n(CCCCCCN2CCN(c3cccc(C(F)(F)F)c3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
4397947 179019 6 None 1 2 Human 4.4 pKi = 4.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 323 3 0 3 2.5 CN(C)CCN1C(=O)c2ccccc2N(C)C(=O)c2ccccc21 10.1016/j.bmcl.2020.127493
CHEMBL4742201 179019 6 None 1 2 Human 4.4 pKi = 4.4 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 323 3 0 3 2.5 CN(C)CCN1C(=O)c2ccccc2N(C)C(=O)c2ccccc21 10.1016/j.bmcl.2020.127493
118736376 118443 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423340 118443 0 None -18 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 531 7 0 9 3.3 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1016/j.ejmech.2015.04.046
162653726 179959 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 272 2 0 4 2.5 CS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
CHEMBL4753752 179959 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 272 2 0 4 2.5 CS(=O)(=O)n1ccc2ccc(-c3ccncc3)cc21 10.1016/j.ejmech.2020.112916
9885982 103707 0 None -1348 2 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptorCompound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 375 3 0 3 4.0 Brc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
CHEMBL309750 103707 0 None -1348 2 Human 5.4 pKi = 5.4 Binding
Compound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptorCompound was tested for its binding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 375 3 0 3 4.0 Brc1ccc2ccn(CCN3CCCN4CCCCC4C3)c2c1 10.1016/s0960-894x(02)00438-9
155551353 173390 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 323 1 1 2 3.2 Cn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4541526 173390 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 323 1 1 2 3.2 Cn1cncc1-c1c[nH]c2ccc(I)cc12 10.1016/j.ejmech.2019.03.017
162662150 180812 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccncc3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4763536 180812 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 334 3 0 4 3.9 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccncc3)ccc21 10.1016/j.ejmech.2020.112916
11522477 93630 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL248985 93630 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.1 COc1ccc(N2CCN(C)CC2)cc1NCc1ccccc1 10.1016/j.bmcl.2007.09.016
44567983 178527 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL471783 178527 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
162656454 180386 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 449 5 1 8 2.8 COc1cccc(S(=O)(=O)n2c(-c3ccccc3)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4758494 180386 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysisDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
ChEMBL 449 5 1 8 2.8 COc1cccc(S(=O)(=O)n2c(-c3ccccc3)nc3c(N4CCNCC4)nccc32)c1 10.1021/acs.jmedchem.0c02009
71463517 84873 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 287 2 1 5 2.2 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260375 84873 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 287 2 1 5 2.2 Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccncc12 10.1007/s00044-004-0121-8
57391729 69403 0 None -5 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69403 0 None -5 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
24784066 175615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 343 3 1 6 2.1 O=S(=O)(c1ccccc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL459349 175615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 343 3 1 6 2.1 O=S(=O)(c1ccccc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
16222759 81615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165531 81615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
11257897 130848 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm049615n
CHEMBL368871 130848 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm049615n
44403080 71078 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
CHEMBL195987 71078 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 2 1 4 3.2 O=S(=O)(c1cccc(Cl)c1)n1c2c(c3ccccc31)CCNC2 10.1016/j.bmcl.2005.07.028
52912979 127380 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127380 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
71454997 80999 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 490 9 1 5 5.1 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159455 80999 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 490 9 1 5 5.1 O=S(=O)(NCC1CCN(CCOc2ccccc2-c2ccccc2)CC1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
156015194 176979 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 377 4 2 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640332 176979 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 377 4 2 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
24893978 995 5 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
8872 995 5 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
CHEMBL495075 995 5 None -1023 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 525 6 2 4 4.9 Brc1cc(ccc1OC1CCNCC1)CN1CC[C@@H](C1)NC(=O)c1ccc(c(c1)Cl)Cl 10.1016/j.bmcl.2008.06.019
90656161 110343 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cncc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260793 110343 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cncc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
164611003 184762 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860006 184762 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
3005573 57139 47 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
CHEMBL1655 57139 47 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 10.1021/jm2011657
134156520 153581 0 None -93 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 501 13 1 5 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3985152 153581 0 None -93 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 501 13 1 5 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
90654831 109338 0 None -758 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 CCOc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233401 109338 0 None -758 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 512 9 0 5 4.4 CCOc1ccccc1N1CCN(CCCN2C(=O)N(C)C(=O)C2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
4011 81996 43 None -28 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -28 23 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
168269921 189487 0 None -1380 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 430 8 0 7 3.4 O=c1n(CCCCCCN2CCN(c3cccc4cccnc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5172673 189487 0 None -1380 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 430 8 0 7 3.4 O=c1n(CCCCCCN2CCN(c3cccc4cccnc34)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
156013588 176627 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 353 3 2 4 2.9 COc1cc2c3c(c1OC)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4635229 176627 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 353 3 2 4 2.9 COc1cc2c3c(c1OC)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
124247485 163517 7 None -4 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4209274 163517 7 None -4 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 231 1 2 2 1.9 Fc1ccc(-c2n[nH]c3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
138691329 170156 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(Cl)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4452121 170156 0 None -100 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 245 2 1 2 3.7 CCn1cncc1-c1c[nH]c2ccc(Cl)cc12 10.1016/j.ejmech.2019.03.017
155551197 173384 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 382 6 2 2 6.4 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)s3)cccc2c1 10.1016/j.ejmech.2019.111857
CHEMBL4541384 173384 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 382 6 2 2 6.4 c1ccc2c(-c3ccc(CNCCc4c[nH]c5ccccc45)s3)cccc2c1 10.1016/j.ejmech.2019.111857
155557661 174078 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 306 6 2 3 4.4 c1coc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4558397 174078 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 306 6 2 3 4.4 c1coc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
44395633 65936 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 362 5 0 4 3.7 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL184671 65936 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 362 5 0 4 3.7 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2004.09.003
145957184 161532 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 5 1 5 3.3 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4160798 161532 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 369 5 1 5 3.3 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
126720444 162200 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 6 1 5 4.1 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4171504 162200 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 377 6 1 5 4.1 CCC(CC)c1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C)c1 10.1016/j.ejmech.2017.12.053
45487100 196126 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 381 4 1 8 2.2 NCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL572087 196126 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 381 4 1 8 2.2 NCCn1cc(S(=O)(=O)c2c(Cl)nc3sccn23)c2ncccc21 10.1016/j.bmcl.2009.10.067
155554955 173748 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.1 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
CHEMBL4550561 173748 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.1 O=S(=O)(c1ccccc1)N1Cc2cccc(C3CCN(C4CCC4)CC3)c2C1 10.1016/j.bmcl.2016.07.055
25263317 173868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 317 4 1 2 4.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL455332 173868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 317 4 1 2 4.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
66801230 111564 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 436 8 1 7 3.2 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289951 111564 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 436 8 1 7 3.2 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
44459048 90550 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 356 4 3 5 2.3 CNc1cc(S(=O)(=O)Nc2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
CHEMBL23965 90550 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 356 4 3 5 2.3 CNc1cc(S(=O)(=O)Nc2ccc(N)cc2)cc(Br)n1 10.1021/jm021085c
44401620 68297 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 241 2 1 2 4.0 Nc1ccc(SC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL191844 68297 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 241 2 1 2 4.0 Nc1ccc(SC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
155568246 175526 0 None -186 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 528 9 2 5 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(OC)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4591440 175526 0 None -186 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 528 9 2 5 5.2 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(OC)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
145962006 161024 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4129055 161024 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
23786472 9450 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 434 8 0 5 4.6 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
CHEMBL112285 9450 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 434 8 0 5 4.6 COc1ccc2c(c1)c(CCN(C)Cc1ccccc1)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(03)00612-7
44403052 69475 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 4 1 4 3.9 O=S(=O)(c1ccccc1Br)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL193657 69475 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 418 4 1 4 3.9 O=S(=O)(c1ccccc1Br)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
68108593 131102 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692844 131102 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccc(F)cc1)c1ccc2oc3c(c2c1)CNCC3 nan
16222764 81616 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165532 81616 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL5093017 213626 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc(F)c(Cl)c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
66800942 111553 0 None -112 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 416 6 1 6 2.7 Cc1cccc(S(=O)(=O)NCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289708 111553 0 None -112 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 416 6 1 6 2.7 Cc1cccc(S(=O)(=O)NCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1021/jm401895u
10994400 203411 0 None -467 4 Human 6.4 pKi = 6.4 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
CHEMBL77855 203411 0 None -467 4 Human 6.4 pKi = 6.4 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 439 5 1 2 4.4 OC(c1ccc(F)cc1)C1CCN(CCc2ccccc2I)CC1 10.1021/jm0200411
164619216 185082 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864863 185082 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
58258845 127426 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 4 2 5 2.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2CCO)CC2CCC1N2 nan
CHEMBL3664772 127426 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 4 2 5 2.8 O=S(=O)(c1ccccc1)c1ccc2c(c1)c1c(n2CCO)CC2CCC1N2 nan
155511929 175703 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4436319 175703 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595069 175703 0 None -2 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
134155645 150541 0 None -30 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3958956 150541 0 None -30 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.7 C[C@@H]1CN(c2ccccc2-c2ccccc2)CCN1CCCCCC(=O)NCc1ccccc1 10.1016/j.ejmech.2016.05.005
24861250 198317 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cellsInhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cells
ChEMBL 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 10.1016/j.bmc.2009.09.023
CHEMBL595252 198317 0 None -7 3 Human 6.4 pKi = 6.4 Binding
Inhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cellsInhibition of [3H]LSD binding to human 5HT6 receptor expressed in human HeLa cells
ChEMBL 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 10.1016/j.bmc.2009.09.023
155522218 170070 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
CHEMBL4451231 170070 0 None -19 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 492 7 1 5 5.3 O=c1c(-c2ccccc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
90654838 112190 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233668 112190 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304237 112190 0 None -63 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 448 9 0 4 4.2 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2014.01.065
52912981 127381 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
CHEMBL3664728 127381 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 382 3 1 5 3.4 COc1ccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)cc1 nan
58258823 127401 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cncc(Cl)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664747 127401 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 387 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4cncc(Cl)c4)ccc31)C1CCC(C2)N1 nan
58258842 128468 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 412 5 2 6 2.7 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCCO)c31)C1CCC(C2)N1 nan
CHEMBL3669667 128468 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 412 5 2 6 2.7 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCCO)c31)C1CCC(C2)N1 nan
44395663 122413 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
CHEMBL360642 122413 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2cc(F)ccc21 10.1016/j.bmcl.2004.09.003
10156876 18638 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 6 0 5 3.5 COc1ccc2c(c1)c(CCN1CCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL127975 18638 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 384 6 0 5 3.5 COc1ccc2c(c1)c(CCN1CCCC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44438729 93422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 293 5 1 3 3.4 CN(C)CCc1cn(Cc2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247885 93422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 293 5 1 3 3.4 CN(C)CCc1cn(Cc2ccc(N)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
53319475 59814 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642868 59814 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739583 59814 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 422 6 2 5 3.4 CN(C)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
16118926 59837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642857 59837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739695 59837 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NCC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
118654518 190930 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
CHEMBL5194172 190930 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 425 4 1 5 3.9 O=S(=O)(c1ccc(Cl)cc1)n1cc(C(F)F)c2cc(N3CCNCC3)ccc21 10.1016/j.bmc.2022.116950
10182052 134667 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 3 1 5 5.5 Cc1c(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
CHEMBL372033 134667 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 444 3 1 5 5.5 Cc1c(S(=O)(=O)n2cc(C3CCCNC3)c3ccccc32)sc2ccc(Cl)cc12 10.1016/j.bmcl.2005.07.028
155526468 170648 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4459485 170648 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.ejmech.2019.06.001
66801251 111628 0 None -16 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 507 7 1 6 5.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3290013 111628 0 None -16 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 507 7 1 6 5.4 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68115866 131723 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1ccc(F)cc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696958 131723 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 349 2 1 4 3.2 O=S(=O)(c1ccc(F)cc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL5077178 212716 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)cc1 10.1021/acs.jmedchem.1c00497
CHEMBL5093250 213645 0 None -3 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)c(F)c1 10.1021/acs.jmedchem.1c00497
44403071 140258 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1cccc(C(F)(F)F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL381871 140258 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.3 O=S(=O)(c1cccc(C(F)(F)F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
274 3287 39 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
5312145 3287 39 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
CHEMBL433461 3287 39 None -1 3 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm049615n
134138168 147158 0 None -39 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147158 0 None -39 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44438716 93419 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 364 11 0 4 4.3 CCCCCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL247871 93419 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 364 11 0 4 4.3 CCCCCCCCS(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
137655929 158402 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
CHEMBL4095896 158402 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 314 4 1 7 0.8 COc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
155552356 173503 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4544262 173503 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2ccc3c(c2)CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
44438731 93423 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 0 2 4.8 CN(C)CCc1cn(Cc2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL247886 93423 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 0 2 4.8 CN(C)CCc1cn(Cc2ccc(C(F)(F)F)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
137650705 156692 0 None -12 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076408 156692 0 None -12 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 498 6 0 5 4.5 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
19958507 98962 0 None -891 5 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL282829 98962 0 None -891 5 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
49780170 16997 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256251 16997 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 811 17 2 9 8.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
118736373 118440 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 545 7 0 9 3.6 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423337 118440 0 None -19 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 545 7 0 9 3.6 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
44401550 69472 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.6 Nc1ccc(CC2C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL193637 69472 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 221 2 1 1 3.6 Nc1ccc(CC2C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
136152964 193270 0 None -1548 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 193270 0 None -1548 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
5206725 153546 13 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 402 6 1 5 4.5 CN1CCN(c2ccc([N+](=O)[O-])c(NC(c3ccccc3)c3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL398481 153546 13 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 402 6 1 5 4.5 CN1CCN(c2ccc([N+](=O)[O-])c(NC(c3ccccc3)c3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12017574 203091 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc(Cl)cc3)c12 10.1016/s0960-894x(00)00453-4
CHEMBL75029 203091 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 392 6 0 5 3.6 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc(Cl)cc3)c12 10.1016/s0960-894x(00)00453-4
9907512 18509 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/jm010943m
CHEMBL127732 18509 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 372 6 0 5 3.3 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc(C)cc1 10.1021/jm010943m
145985823 165371 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250475 165371 0 None -22 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 6 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1016/j.ejmech.2018.01.002
145963274 161034 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4129259 161034 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 407 3 1 5 3.9 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
45484352 196959 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL579063 196959 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 347 5 0 5 2.6 CN(C)CCn1cc(S(=O)(=O)c2ccc(F)cc2)c2cccnc21 10.1016/j.bmc.2009.05.055
45484339 197225 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 389 5 0 5 3.6 O=S(=O)(c1cccc(Cl)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
CHEMBL584474 197225 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 389 5 0 5 3.6 O=S(=O)(c1cccc(Cl)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
155562755 174631 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4571059 174631 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
71151767 117738 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4F)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409239 117738 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 526 9 1 5 5.7 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4ccccc4F)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118736374 118441 0 None -5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 559 8 0 9 4.0 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423338 118441 0 None -5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 559 8 0 9 4.0 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(-c4ccccc4)cn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
66801605 111573 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 520 8 1 7 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289960 111573 0 None -6 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 520 8 1 7 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68115766 131215 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)C(=O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692956 131215 0 None - 1 Human 7.4 pKi = 7.4 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)C(=O)CN1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
25263311 184066 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484964 184066 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
125513586 162327 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)nccc32)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4173336 162327 2 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 293 3 1 5 1.9 c1ccc(Cn2cnc3c(N4CCNCC4)nccc32)cc1 10.1016/j.ejmech.2017.12.053
11232643 132952 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1cn2c3c(cccc13)-c1ccccc1S2(=O)=O 10.1016/j.bmcl.2006.08.068
CHEMBL3706857 132952 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.0 CN(C)CCc1cn2c3c(cccc13)-c1ccccc1S2(=O)=O 10.1016/j.bmcl.2006.08.068
155535154 171476 0 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 556 9 1 7 5.2 COc1ccc(-c2c3n(c(=O)n(CCCCN4CCCC(c5c[nH]c6ccc(OC)cc56)C4)c2=O)CCCC3)cc1 10.1016/j.ejmech.2019.07.027
CHEMBL4471755 171476 0 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 556 9 1 7 5.2 COc1ccc(-c2c3n(c(=O)n(CCCCN4CCCC(c5c[nH]c6ccc(OC)cc56)C4)c2=O)CCCC3)cc1 10.1016/j.ejmech.2019.07.027
52912979 127380 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127380 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
71574306 85839 0 None -26 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
CHEMBL2312639 85839 0 None -26 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
155557500 174074 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4558215 174074 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 488 6 2 6 5.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccc4ccccc4c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
145985224 164936 0 None -114 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240162 164936 0 None -114 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1cccc2ncccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
145972025 163927 0 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 409 4 1 3 4.1 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4214208 163927 0 None -16 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 409 4 1 3 4.1 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168284840 190702 0 None -147 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 439 5 0 6 3.8 O=c1n(CC2CCC(CN3CCN(c4cccc(Cl)c4)CC3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
CHEMBL5190996 190702 0 None -147 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 439 5 0 6 3.8 O=c1n(CC2CCC(CN3CCN(c4cccc(Cl)c4)CC3)CC2)nc2ccccn12 10.1016/j.ejmech.2022.114319
57399093 68097 0 None -138 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 443 9 0 4 4.9 CCN(CCCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
CHEMBL1917360 68097 0 None -138 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 443 9 0 4 4.9 CCN(CCCCCN1CCC2CCCCC2C1)S(=O)(=O)c1cccc2cccnc12 10.1016/j.bmc.2011.09.044
52912977 127379 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664726 127379 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 420 2 1 4 4.4 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)ccc31)C1CCC(C2)N1 nan
44397550 70848 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL188285 70848 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL195621 70848 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
44395632 121836 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2004.09.003
CHEMBL359967 121836 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2004.09.003
1574 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
218 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
CHEMBL266591 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm990550b
20901207 10882 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
CHEMBL1173508 10882 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 359 2 1 8 2.4 Cc1ccc(C)c(S(=O)(=O)c2nnn3c2nc(N)c2sccc23)c1 10.1016/j.bmc.2010.05.051
1574 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
218 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
CHEMBL266591 81 52 None 1 20 Human 7.3 pKi = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptorBinding affinity towards 5-hydroxytryptamine 6 receptor
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm030030n
44568020 183353 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL481472 183353 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1ccc(C(F)(F)F)cc1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
56944955 159144 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
CHEMBL4104216 159144 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 465 6 2 3 5.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1cccc2ccccc12 10.1021/acs.jmedchem.7b00839
57400477 69398 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935588 69398 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CCNC3 10.1016/j.bmcl.2011.11.050
24763355 62297 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 4 4.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783604 62297 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 423 3 1 4 4.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(C(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
45487099 196014 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1cccc(S(=O)(=O)c2cn(CCN)c3cccnc23)c1 10.1016/j.bmcl.2009.10.067
CHEMBL571215 196014 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 315 4 1 5 2.1 Cc1cccc(S(=O)(=O)c2cn(CCN)c3cccnc23)c1 10.1016/j.bmcl.2009.10.067
56944186 111598 0 None -8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 8 1 7 4.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289984 111598 0 None -8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 504 8 1 7 4.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
68108804 131167 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
CHEMBL3692908 131167 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 362 2 1 4 3.8 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CC(O)CC3 nan
90644513 111204 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286588 111204 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
11501251 93939 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 6 1 5 2.9 COC(=O)c1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
CHEMBL250804 93939 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 6 1 5 2.9 COC(=O)c1ccc(N2CCN(C)CC2)cc1NCCc1ccccc1 10.1016/j.bmcl.2007.09.016
165193 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3138 60 None -158 42 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
164628531 185882 0 None 5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4876727 185882 0 None 5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
44404394 132294 0 None -41 7 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL370128 132294 0 None -41 7 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
44386469 130156 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 428 6 0 6 3.9 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL368294 130156 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 428 6 0 6 3.9 COc1ccc(S(=O)(=O)n2c3c(c4cc(OC)ccc42)C(CN(C)C)CCC3)cc1 10.1016/j.bmcl.2004.01.071
46214153 110206 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
CHEMBL3260334 110206 0 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
ChEMBL 367 5 1 3 4.0 Clc1cccc(COc2ccc(Br)cc2OC2CNC2)c1 10.1021/ml500082j
90644513 111204 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286588 111204 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 351 2 1 5 1.9 O=S(=O)(C1=CC=C=C=C1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm8009469
23655464 88957 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 330 5 1 5 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL236986 88957 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 330 5 1 5 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
90656168 110350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260801 110350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 342 2 1 3 3.7 O=C1OC(c2ccccc2Cl)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
66800934 111562 0 None -21 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 9 1 7 4.1 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289949 111562 0 None -21 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 9 1 7 4.1 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
68115856 131744 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 398 3 1 6 2.7 O=S(=O)(c1ccccc1)c1cc(N2CCOCC2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696979 131744 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 398 3 1 6 2.7 O=S(=O)(c1ccccc1)c1cc(N2CCOCC2)c2oc3c(c2c1)CNCC3 nan
127032424 138581 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786703 138581 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 398 4 1 4 2.9 CCN/C(=N\S(=O)(=O)c1cc(Cl)cc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
168268877 189377 0 None -10 12 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189377 0 None -10 12 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
164624803 185630 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873127 185630 0 None 2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164613297 184034 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4849230 184034 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cc(Cl)ccc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
122377930 136129 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1016/j.ejmech.2015.11.040
CHEMBL3740054 136129 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1016/j.ejmech.2015.11.040
122377930 136129 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1039/C5MD00166H
CHEMBL3740054 136129 0 None -52 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 420 8 1 4 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc(F)c2)CC1 10.1039/C5MD00166H
162651238 179686 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 238 2 0 4 1.5 CN(C)c1cccc2c1ccn2S(C)(=O)=O 10.1016/j.ejmech.2020.112916
CHEMBL4750554 179686 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 238 2 0 4 1.5 CN(C)c1cccc2c1ccn2S(C)(=O)=O 10.1016/j.ejmech.2020.112916
168275477 189857 0 None -263 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 388 9 5 7 3.1 Nc1nc(NCCNc2ccccc2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5178499 189857 0 None -263 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 388 9 5 7 3.1 Nc1nc(NCCNc2ccccc2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
145969402 164266 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4218625 164266 0 None -165 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 410 4 1 4 3.1 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
162644287 181208 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2020.112916
CHEMBL4777921 181208 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2020.112916
145975720 163408 0 None -229 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 394 4 1 4 2.5 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4207835 163408 0 None -229 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 394 4 1 4 2.5 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
168268929 189437 0 None 3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 456 9 5 7 4.4 Nc1nc(NCCNc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5171734 189437 0 None 3 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 456 9 5 7 4.4 Nc1nc(NCCNc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155515399 169390 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.9 CC(Cc1c[nH]c2ccccc12)NCc1ccc(-c2ccc(O)cc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4441691 169390 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.9 CC(Cc1c[nH]c2ccccc12)NCc1ccc(-c2ccc(O)cc2)o1 10.1016/j.ejmech.2019.111857
155557134 173965 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 493 10 0 5 5.1 CCOc1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4555890 173965 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 493 10 0 5 5.1 CCOc1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
118464425 137781 0 None -125 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 137781 0 None -125 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
58258834 128439 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 429 3 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669638 128439 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 429 3 1 5 4.4 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-c5ccncc5)c4)ccc31)C1CCC(C2)N1 nan
44403088 140420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL382297 140420 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 406 3 1 4 4.6 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
24763429 62298 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 4 1 5 4.1 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783605 62298 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 439 4 1 5 4.1 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
127047899 139281 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3cccc(C(F)(F)F)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798840 139281 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 480 5 0 6 4.3 CC(C)CS(=O)(=O)n1ccc2c(-c3cccc(C(F)(F)F)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
44242965 18574 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
CHEMBL1277916 18574 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 392 3 2 5 3.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(N3CCNCC3)c12 10.1021/jm1007825
90656160 110342 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)n1 10.1016/j.bmcl.2014.03.049
CHEMBL3260792 110342 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 322 3 1 4 2.0 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)n1 10.1016/j.bmcl.2014.03.049
57395082 71200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949766 71200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1963006 71200 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.4 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
56944191 111610 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 483 8 1 5 4.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289996 111610 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 483 8 1 5 4.7 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
25263334 178897 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 4.0 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1ccccc1 10.1016/j.bmcl.2009.03.077
CHEMBL474089 178897 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 4.0 Cc1c(C2CCNCC2)ccnc1O[C@@H](C)c1ccccc1 10.1016/j.bmcl.2009.03.077
45378935 197824 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591939 197824 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 434 4 1 6 4.1 CC(C)n1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
11729823 102498 1 None -95 5 Human 7.3 pKi = 7.3 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2cccc(I)c2)CC1 10.1021/jm0200411
CHEMBL306478 102498 1 None -95 5 Human 7.3 pKi = 7.3 Binding
Tested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSDTested on cell membranes from transfected cells selectively expressing human 5-hydroxytryptamine 6 receptor incubated with 1 nM [3H]LSD
ChEMBL 437 5 0 2 4.6 O=C(c1ccc(F)cc1)C1CCN(CCc2cccc(I)c2)CC1 10.1021/jm0200411
134145903 148346 0 None -47 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3941529 148346 0 None -47 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
155541872 176111 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4519312 176111 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598357 176111 0 None -11 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
68281137 111588 0 None -22 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 9 1 7 3.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289974 111588 0 None -22 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 9 1 7 3.6 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
11630824 93904 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 4 1 6 2.0 CN1CCN(c2ccc([N+](=O)[O-])c(Nn3cccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL250661 93904 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 4 1 6 2.0 CN1CCN(c2ccc([N+](=O)[O-])c(Nn3cccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
227584 157951 36 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4091082 157951 36 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 229 2 1 2 1.9 CN1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
2771418 153631 32 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 1 6 1.8 Cc1cc(C)n(-c2cc(N3CCNCC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
CHEMBL398555 153631 32 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 1 6 1.8 Cc1cc(C)n(-c2cc(N3CCNCC3)ccc2[N+](=O)[O-])n1 10.1016/j.bmcl.2007.09.016
164618100 184778 0 None 5 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 184778 0 None 5 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
71574300 85859 0 None -20 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312937 85859 0 None -20 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ncccc2c1 10.1016/j.ejmech.2012.11.042
162645383 179038 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4742713 179038 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3c(ccn3S(=O)(=O)c3ccccc3)c2)CC1 10.1016/j.ejmech.2020.112916
155562063 175178 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 8 2 3 5.5 CC(C)Oc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4583433 175178 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 374 8 2 3 5.5 CC(C)Oc1cccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
156017281 177091 0 None -489 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 466 8 0 6 4.0 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4641609 177091 0 None -489 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 466 8 0 6 4.0 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
156018141 177347 0 None -1230 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 439 9 0 5 3.4 COc1ccccc1N1CCN(CCCCCCN2C(=O)[C@H]3[C@@H]4CC[C@@H](C4)[C@H]3C2=O)CC1 10.1016/j.bmc.2020.115459
CHEMBL4645292 177347 0 None -1230 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 439 9 0 5 3.4 COc1ccccc1N1CCN(CCCCCCN2C(=O)[C@H]3[C@@H]4CC[C@@H](C4)[C@H]3C2=O)CC1 10.1016/j.bmc.2020.115459
164620867 185060 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4864448 185060 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 410 6 1 7 3.4 CCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
162666403 181810 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 306 3 0 4 3.2 CN(C)c1cccc2c1ccn2S(=O)(=O)C1CCCCC1 10.1016/j.ejmech.2020.112916
CHEMBL4785319 181810 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 306 3 0 4 3.2 CN(C)c1cccc2c1ccn2S(=O)(=O)C1CCCCC1 10.1016/j.ejmech.2020.112916
49783209 17427 0 None -851 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17427 0 None -851 27 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44581972 175027 0 None -16 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175027 0 None -16 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
138691366 174386 0 None -16 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2ccc(F)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4565881 174386 0 None -16 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2ccc(F)cc12 10.1016/j.ejmech.2019.03.017
23857192 83972 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL2113365 83972 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
CHEMBL2219584 83972 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 322 2 1 4 3.6 Nc1ccc(S(=O)(=O)n2c3ccccc3c3ccccc32)cc1 10.1016/j.bmcl.2004.01.071
44403056 70215 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1ccc(Cl)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL194834 70215 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 374 4 1 4 3.8 O=S(=O)(c1ccc(Cl)cc1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403066 168058 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 4 1 4 4.5 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL436124 168058 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 408 4 1 4 4.5 O=S(=O)(c1ccc(Cl)c(Cl)c1)n1cc(C[C@@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.07.028
10342674 6087 4 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)CC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081074 6087 4 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 430 5 0 4 5.3 O=S(=O)(c1ccccc1)c1cn(C2CCN(Cc3ccccc3)CC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
145960391 160856 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4126633 160856 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1cccc(Cl)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
24777061 94421 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
CHEMBL253826 94421 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
137636699 155626 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 3 2 3 2.3 NC1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
CHEMBL4063897 155626 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 302 3 2 3 2.3 NC1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/acs.jmedchem.7b00085
45488166 195237 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
CHEMBL566219 195237 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 342 3 2 3 3.7 c1ccc2cc(Cc3nc4c(N5CCNCC5)cccc4[nH]3)ccc2c1 10.1021/jm901672k
57391669 71218 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949677 71218 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963079 71218 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
56593803 65360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
CHEMBL1834346 65360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 370 5 1 3 3.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)(CC)C=N1 10.1021/jm200466r
11811724 116401 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 413 6 0 6 2.7 COc1ccc2c(c1)c(CCN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL338380 116401 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 413 6 0 6 2.7 COc1ccc2c(c1)c(CCN1CCN(C)CC1)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
118731510 117744 0 None -16 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 9 1 4 5.4 NC(=O)c1ccccc1OCCCN1CCC(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409245 117744 0 None -16 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 467 9 1 4 5.4 NC(=O)c1ccccc1OCCCN1CCC(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
71463520 84876 2 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 2 2 1.6 CCc1[nH]c2ccncc2c1CCN 10.1007/s00044-004-0121-8
CHEMBL2260378 84876 2 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 189 3 2 2 1.6 CCc1[nH]c2ccncc2c1CCN 10.1007/s00044-004-0121-8
90656164 110346 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 2 1 4 1.8 O=C1CCCN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260797 110346 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 2 1 4 1.8 O=C1CCCN1c1cnc2c(N3CCNCC3)cccc2c1 10.1016/j.bmcl.2014.03.049
135367857 164052 0 None -30 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 164052 0 None -30 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
57414790 131211 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 425 3 0 5 3.2 CS(=O)(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692952 131211 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 425 3 0 5 3.2 CS(=O)(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
168291393 191396 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 338 8 2 3 2.7 NC(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5201464 191396 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 338 8 2 3 2.7 NC(=O)NCCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
155520499 169916 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 494 9 0 6 4.6 O=[N+]([O-])c1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4449148 169916 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 494 9 0 6 4.6 O=[N+]([O-])c1ccccc1N1CCN(CCCCCCN2c3cccc4cccc(c34)S2(=O)=O)CC1 10.1016/j.bmcl.2019.06.029
145985585 165336 0 None -165 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249640 165336 0 None -165 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
162652195 179766 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 280 5 0 4 2.7 CCCCS(=O)(=O)n1ccc2c(N(C)C)cccc21 10.1016/j.ejmech.2020.112916
CHEMBL4751332 179766 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 280 5 0 4 2.7 CCCCS(=O)(=O)n1ccc2c(N(C)C)cccc21 10.1016/j.ejmech.2020.112916
44386911 130819 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 432 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Cl)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL368746 130819 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 432 5 0 5 4.5 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(Cl)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
6918647 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
CHEMBL292759 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm5003952
58258756 127435 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127435 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
6918647 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.01.031
CHEMBL292759 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.01.031
12017577 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2004.05.076
CHEMBL72554 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/j.bmcl.2004.05.076
9929294 63749 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL180765 63749 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 370 3 0 4 3.7 CN1CC=C(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
44388970 64525 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL182099 64525 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 396 3 1 7 3.3 O=S(=O)(c1nccc2sncc12)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
12017577 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/s0960-894x(00)00453-4
CHEMBL72554 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1016/s0960-894x(00)00453-4
44395595 66743 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
CHEMBL187278 66743 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 314 5 1 4 2.6 CNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.09.003
67156504 161601 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4161904 161601 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
145973178 162546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
CHEMBL4177024 162546 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 343 3 1 7 1.1 O=S(=O)(c1ccccc1)n1ncc2c(N3CCNCC3)nccc21 10.1016/j.ejmech.2017.12.053
6918647 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm030030n
CHEMBL292759 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm030030n
12017577 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm030030n
CHEMBL72554 202795 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 408 6 0 5 4.1 COc1cccc2c(CCN(C)C)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm030030n
2876391 206470 93 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 140 0 1 2 0.4 C1CCN2CCNCC2C1 10.1021/jm030030n
CHEMBL98511 206470 93 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 140 0 1 2 0.4 C1CCN2CCNCC2C1 10.1021/jm030030n
137636384 155410 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 356 4 0 4 2.5 CN(C)CC1=CC2=CN(S(=O)(=O)c3ccccc3)C3=CC=CC(O1)C23 10.1021/acsmedchemlett.6b00482
CHEMBL4061189 155410 0 None 12 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 356 4 0 4 2.5 CN(C)CC1=CC2=CN(S(=O)(=O)c3ccccc3)C3=CC=CC(O1)C23 10.1021/acsmedchemlett.6b00482
135398745 2869 108 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
47 2869 108 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
CHEMBL715 2869 108 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
DB00334 2869 108 None -4 65 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2012.07.043
155534670 171399 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4470718 171399 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1cncc2ccccc12)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
155513438 169162 0 None 4 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.8 Cc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4438434 169162 0 None 4 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 346 6 3 3 4.8 Cc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(O)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
164618879 185308 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4868468 185308 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 426 3 1 6 3.5 O=S(=O)(c1ccccc1Cl)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
10319820 160648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4073586 160648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117715 160648 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 5 0 6 2.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
2435 3533 78 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
60149 3533 78 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
98 3533 78 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
CHEMBL12713 3533 78 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
DB06144 3533 78 None -9 48 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1016/j.bmcl.2010.07.105
44397689 71096 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196102 71096 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL373107 71096 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10272325 71397 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL196619 71397 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 5 0 6 3.3 COc1ccc(S(=O)(=O)n2cc(C3CCN(C)C3)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
44403099 132489 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL370215 132489 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 368 4 0 4 3.8 Cc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44435617 88712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236579 88712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
9840311 5475 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1076665 5475 4 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 326 3 1 4 3.0 O=S(=O)(c1ccccc1)c1cn(C2CCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
46880658 6303 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1082199 6303 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 376 3 0 4 3.6 CN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cc(F)ccc32)C1 10.1016/j.bmcl.2010.01.073
164613324 184094 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4849917 184094 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 440 8 1 5 4.7 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3cccc(Cl)c3)cccc21 10.1016/j.ejmech.2021.113792
127046819 139222 0 None 75 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 451 5 1 6 3.8 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc4[nH]ccc4c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798478 139222 0 None 75 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 451 5 1 6 3.8 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc4[nH]ccc4c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
57400234 71196 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1949928 71196 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
CHEMBL1962959 71196 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 383 2 1 4 3.7 O=S(=O)(c1ccc2c(c1)O[C@H]1CNCC[C@@H]21)c1cccc(Cl)c1Cl 10.1016/j.bmcl.2011.12.026
56944564 111567 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289954 111567 0 None -5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 480 8 1 6 4.3 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
11396708 200525 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
CHEMBL609739 200525 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Br)cc12 10.1021/jm049243i
11316594 200556 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
CHEMBL609993 200556 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 439 6 3 4 4.2 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(OC(F)(F)F)cc1 10.1021/jm049243i
68108945 131110 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)c1cccc2ccccc12 nan
CHEMBL3692852 131110 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 363 2 1 4 4.1 O=S(=O)(c1ccc2oc3c(c2c1)CNCC3)c1cccc2ccccc12 nan
71462329 81623 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 406 3 0 4 4.1 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165539 81623 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 406 3 0 4 4.1 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2cccc(Cl)c2)C1 10.1016/j.bmcl.2012.06.002
17940268 50015 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)c(Cl)cc2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL157175 50015 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 449 5 2 5 3.9 COc1ccc(S(=O)(=O)Nc2cc(Cl)c(Cl)cc2Cl)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
44328748 205959 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@H](C)N[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95511 205959 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 500 4 2 6 5.4 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4C[C@H](C)N[C@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
6918647 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 100278 2 None 50 14 Human 8.3 pKi = 8.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
44398251 67682 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1cccc2c(CCN)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm050247c
CHEMBL191385 67682 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 380 5 1 5 3.5 COc1cccc2c(CCN)cn(S(=O)(=O)c3ccc4ccccc4c3)c12 10.1021/jm050247c
44435617 88712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236579 88712 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccc(F)cc3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
162661903 180846 0 None -14 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
CHEMBL4764006 180846 0 None -14 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
46890293 7238 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 2 3 3.8 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ccc[nH]1 10.1016/j.bmcl.2010.03.110
CHEMBL1086114 7238 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 412 5 2 3 3.8 O=C(NC[C@@H]1CCCc2cc(S(=O)(=O)c3cccc(F)c3)ccc21)c1ccc[nH]1 10.1016/j.bmcl.2010.03.110
46889327 7265 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 359 3 2 4 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc(F)cc4[nH]cnc34)ccc21 10.1016/j.bmcl.2010.03.110
CHEMBL1086251 7265 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 359 3 2 4 2.9 NC[C@@H]1CCCc2cc(S(=O)(=O)c3cc(F)cc4[nH]cnc34)ccc21 10.1016/j.bmcl.2010.03.110
17978376 69145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 3 1 6 2.8 N#Cc1ccc2c(ccn2S(=O)(=O)c2cccc(Cl)c2)c1N1CCNCC1 10.1016/j.bmcl.2005.06.107
CHEMBL193379 69145 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 400 3 1 6 2.8 N#Cc1ccc2c(ccn2S(=O)(=O)c2cccc(Cl)c2)c1N1CCNCC1 10.1016/j.bmcl.2005.06.107
44441241 168358 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 1 4 3.8 CC1(C)CN(S(=O)(=O)c2cccc(F)c2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
CHEMBL438675 168358 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 422 3 1 4 3.8 CC1(C)CN(S(=O)(=O)c2cccc(F)c2)c2cc(F)cc(C3CCNCC3)c2O1 10.1016/j.bmcl.2006.12.093
10216820 85518 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL230069 85518 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 440 4 1 3 5.1 Cc1cc(S(=O)(=O)Nc2ccc3c(c2)CCN(C)CC3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2006.10.036
10173403 86003 0 None 3 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 426 4 1 3 4.8 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231430 86003 0 None 3 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 426 4 1 3 4.8 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
44425699 150035 6 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 1 3 3.8 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CN(C)C3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL395501 150035 6 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 344 6 1 3 3.8 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CN(C)C3)cc1 10.1016/j.bmcl.2006.10.036
9892409 100483 0 None 63 9 Human 8.3 pKi = 8.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 100483 0 None 63 9 Human 8.3 pKi = 8.3 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]5-LSD as radioligand; n=3
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
71451603 81632 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165547 81632 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 450 3 0 4 4.2 CN(C)C1CCc2c(c3cc(F)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
135398737 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -4 91 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44386821 61239 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc3ccccc3c2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL177107 61239 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 448 5 0 5 5.0 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc3ccccc3c2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
58258833 127446 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127446 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
66801160 111560 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3289947 111560 0 None 1 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 468 7 1 6 3.6 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68109436 131123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccccc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692865 131123 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1ccccc1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
68115681 131206 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
CHEMBL3692947 131206 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 C[C@H](O)c1cccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)c1 nan
56593932 65362 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
CHEMBL1834348 65362 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 382 3 1 3 3.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCCC2 10.1021/jm200466r
10068007 18600 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278090 18600 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(F)cc4)c3c2)CC1 10.1021/jm1007825
44474625 13957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL1197521 13957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
CHEMBL575270 13957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 451 4 4 7 2.7 CC1(C)C/C(=N\NC(=N)N)c2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm900796p
10113751 61784 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm5003952
CHEMBL177605 61784 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm5003952
10202396 60158 3 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
CHEMBL175471 60158 3 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 2 3 5.0 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc12 10.1021/jm049615n
10113751 61784 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL177605 61784 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 433 5 2 4 5.2 Cc1c(S(=O)(=O)Nc2ccc3[nH]cc(CN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
44544599 177642 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 3 1 6 2.4 CC(=O)N1CCc2ccc(NS(=O)(=O)c3c(Cl)nc4n3CCS4)cc21 10.1016/j.ejmech.2018.11.017
CHEMBL4649783 177642 0 None - 1 Human 8.3 pKi = 8.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 398 3 1 6 2.4 CC(=O)N1CCc2ccc(NS(=O)(=O)c3c(Cl)nc4n3CCS4)cc21 10.1016/j.ejmech.2018.11.017
71502632 117761 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 493 8 0 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409262 117761 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 493 8 0 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
68115685 131190 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1CO nan
CHEMBL3692931 131190 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 3.1 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1CO nan
16049388 81611 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165527 81611 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 384 4 0 5 3.3 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccccc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
44435609 153868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL398808 153868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
20901117 10576 3 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1170672 10576 3 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 399 4 1 8 3.5 O=S(=O)(c1ccccc1)c1nnn2c1nc(NC1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
44435609 153868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL398808 153868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 361 3 1 5 3.1 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
16222652 81627 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 500 3 0 4 5.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165542 81627 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 500 3 0 4 5.1 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
10380133 196659 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL576315 196659 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 301 4 1 5 1.8 NCCn1cc(S(=O)(=O)c2ccccc2)c2cccnc21 10.1016/j.bmc.2009.05.055
49836508 18583 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
CHEMBL1277998 18583 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 374 3 1 5 2.3 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccccc4F)c3c2)CC1 10.1021/jm1007825
1588 2294 24 None -30 43 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2294 24 None -30 43 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2294 24 None -30 43 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2294 24 None -30 43 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2294 24 None -30 43 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
25024524 62605 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
CHEMBL1784917 62605 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.3 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(Cl)c3Cl)c2)CC1 10.1021/ml100101u
129103318 166760 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
CHEMBL4293999 166760 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.ejmech.2020.112709
129103318 166760 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 166760 0 None -7 14 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
25024928 62638 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 5 3.2 O=S(=O)(c1ccc(F)cc1F)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785071 62638 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 5 3.2 O=S(=O)(c1ccc(F)cc1F)n1cc(Cl)c2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
58258785 127404 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5c(F)cccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664750 127404 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 409 2 1 5 3.9 Cn1c2c(c3cc(S(=O)(=O)n4ccc5c(F)cccc54)ccc31)C1CCC(C2)N1 nan
129103161 166517 0 None -51 13 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.bmcl.2021.127909
CHEMBL4289498 166517 0 None -51 13 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 461 6 0 5 4.6 O=C(CCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1016/j.bmcl.2021.127909
56593646 65352 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834338 65352 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 358 4 1 3 2.8 CCN/C(=N\S(=O)(=O)c1cccc2ccccc12)N1CC(CC)C=N1 10.1021/jm200466r
44435615 88711 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236578 88711 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
57398718 69402 0 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
CHEMBL1935592 69402 0 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 343 3 1 5 2.9 COc1cccc(S(=O)(=O)c2ccc3c4c(oc3c2)CNCC4)c1 10.1016/j.bmcl.2011.11.050
46880607 5897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
CHEMBL1079977 5897 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 391 3 1 5 3.9 O=S(=O)(c1cn(C2CCCNC2)c2ccccc12)c1cccc2cccnc12 10.1016/j.bmcl.2010.01.073
68115642 131205 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
CHEMBL3692946 131205 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 391 3 2 5 3.6 CC(O)c1ccc(S(=O)(=O)c2cc(Cl)c3oc4c(c3c2)CNCC4)cc1 nan
68115771 131221 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1ccc(C2CCOC2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692962 131221 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 417 3 1 5 4.1 O=S(=O)(c1ccc(C2CCOC2)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
44435615 88711 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236578 88711 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 359 3 0 5 2.9 CN1CCC(n2cc(S(=O)(=O)c3ccccc3F)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
11350253 113668 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 405 3 1 6 3.0 O=c1n(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm5003952
CHEMBL3329437 113668 0 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 405 3 1 6 3.0 O=c1n(C2=CCNCC2)c2ccccc2n1S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm5003952
44395451 65931 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184652 65931 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 364 5 1 4 3.8 CNCCn1cc(S(=O)(=O)c2cccc3ccccc23)c2ccccc21 10.1016/j.bmcl.2004.09.003
45113530 14108 2 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1095274 14108 2 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
CHEMBL1199079 14108 2 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human recombinant 5HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor by radioligand displacement assay
ChEMBL 340 2 0 4 3.0 CN1CCc2c(c3cc(S(=O)(=O)c4ccccc4)ccc3n2C)C1 10.1016/j.ejmech.2009.10.035
137648172 157268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
CHEMBL4083289 157268 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccccc1Br 10.1021/acs.jmedchem.6b01662
137628796 160442 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4105377 160442 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116137 160442 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 6 1 6 3.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(C(C)C)cc1 10.1021/acs.jmedchem.6b01662
44435626 154319 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
CHEMBL400608 154319 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.bmc.2007.06.024
9865474 174547 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
CHEMBL45695 174547 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 395 3 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2ccc(N3CCN4CCCCC4C3)cc21 10.1016/s0960-894x(00)00320-6
68115878 131737 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 3 2 5 3.0 CC(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696972 131737 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 3 2 5 3.0 CC(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
54580442 62606 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.0 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
CHEMBL1784918 62606 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 451 5 0 5 4.0 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3cccc(C(F)(F)F)c3)c2)CC1 10.1021/ml100101u
44435626 154319 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.ejmech.2010.05.045
CHEMBL400608 154319 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 378 3 1 6 3.0 O=S(=O)(c1cn(C2CCNC2)c2ncccc12)c1cccc2cccnc12 10.1016/j.ejmech.2010.05.045
162657983 180466 0 None -23 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
CHEMBL4759492 180466 0 None -23 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2cc(S(=O)(=O)N[C@@H]3CCN(CCCc4noc5ccccc45)C3)ccc21 10.1016/j.ejmech.2020.112149
52913220 127387 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 4 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664733 127387 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 4 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)F)c4)ccc31)C1CCC(C2)N1 nan
68341955 127427 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5cc[nH]c5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664774 127427 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 391 2 2 4 3.8 Cn1c2c(c3cc(S(=O)(=O)c4ccc5cc[nH]c5c4)ccc31)C1CCC(C2)N1 nan
58258833 127446 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664793 127446 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 419 3 1 5 4.3 CCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
58158739 138627 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3787201 138627 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 350 3 2 4 1.9 CCN/C(=N\S(=O)(=O)c1ccc(O)cc1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
25263347 183544 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccccc2Cl)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482737 183544 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 365 4 1 4 3.9 Cc1c(OS(=O)(=O)c2ccccc2Cl)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
25025314 62603 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 6 0 5 4.1 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C(C)C)cc3)c2)CC1 10.1021/ml100101u
CHEMBL1784915 62603 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 6 0 5 4.1 CCN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccc(C(C)C)cc3)c2)CC1 10.1021/ml100101u
16222866 81642 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 398 4 0 5 3.6 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165557 81642 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 398 4 0 5 3.6 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCC(N(C)C)C1 10.1016/j.bmcl.2012.06.002
68115651 131186 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692927 131186 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 399 2 1 4 4.1 O=S(=O)(c1cccc(C(F)(F)F)c1)c1cc(F)c2oc3c(c2c1)CNCC3 nan
44388980 64164 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 459 6 2 6 4.4 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL181425 64164 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 459 6 2 6 4.4 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(OCc4ccccc4)ccc32)cc1 10.1016/j.bmcl.2004.10.064
44401465 69509 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 293 5 1 3 3.4 CN(C)CCn1cc(Cc2ccc(N)cc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL193841 69509 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 293 5 1 3 3.4 CN(C)CCn1cc(Cc2ccc(N)cc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
5 139 66 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 66 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 66 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 66 None -169 54 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5-HT6 receptor by radioligand displacement assayBinding affinity to human 5-HT6 receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
11849199 77529 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL209383 77529 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
6918531 111741 10 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 365 3 3 3 3.3 Nc1ccc(S(=O)(=O)Nc2cc(Br)cc3[nH]ccc23)cc1 10.1021/jm030030n
CHEMBL329075 111741 10 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 365 3 3 3 3.3 Nc1ccc(S(=O)(=O)Nc2cc(Br)cc3[nH]ccc23)cc1 10.1021/jm030030n
44568063 182431 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 0 5 3.3 CCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
CHEMBL479374 182431 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 0 5 3.3 CCN1CCc2c(n(S(=O)(=O)c3cccc(OC)c3)c3ccccc23)CC1 10.1016/j.bmcl.2008.06.030
162645783 179020 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 11 1 7 5.1 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4742220 179020 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 582 11 1 7 5.1 C#CCNC1CCc2c(OCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
137629291 160461 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4079871 160461 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116243 160461 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 5 1 6 3.5 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3cc(O)ccc32)cc1 10.1021/acs.jmedchem.6b01662
54583109 62204 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
CHEMBL1782358 62204 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1cccc(Sc2ccc3c(c2)N2CCNCC2C3)c1 10.1016/j.bmcl.2010.07.105
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/s0960-894x(00)00320-6
11849199 77529 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL209383 77529 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 261 4 1 3 2.0 NCCc1cccc(S(=O)(=O)c2ccccc2)c1 10.1021/acs.jmedchem.7b00085
155522487 170110 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 428 5 2 6 3.4 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4451666 170110 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 428 5 2 6 3.4 COc1ccc2c(c1)c(-c1cnc(NC(C)=O)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155556757 175690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
CHEMBL4557068 175690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
CHEMBL4594991 175690 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 375 3 1 4 3.0 O=S(=O)(c1ccccc1)n1cc(-c2c[n+]3cccnc3[nH]2)c2ccccc21 10.1016/j.ejmech.2019.06.001
24763354 62295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 369 3 1 4 3.5 Cc1cccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)c1 10.1016/j.bmcl.2009.04.108
CHEMBL1783602 62295 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 369 3 1 4 3.5 Cc1cccc(S(=O)(=O)c2ccc3[nH]nc(C4CCN(C)CC4)c3c2)c1 10.1016/j.bmcl.2009.04.108
25263298 183543 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2c(cnn2S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.bmcl.2009.03.071
CHEMBL482736 183543 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1ccc2c(cnn2S(=O)(=O)c2cccc3ccccc23)c1 10.1016/j.bmcl.2009.03.071
25263330 180425 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1ccc(Cl)cc1 10.1016/j.bmcl.2009.03.077
CHEMBL475902 180425 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1ccc(Cl)cc1 10.1016/j.bmcl.2009.03.077
68115775 131724 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 374 2 1 5 3.1 N#Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696959 131724 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 374 2 1 5 3.1 N#Cc1cc(S(=O)(=O)c2cc(F)cc(F)c2)cc2c3c(oc12)CCNC3 nan
11307899 78458 0 None -794 7 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
CHEMBL2112882 78458 0 None -794 7 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells using [3H]LSD as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm980532e
6918515 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
71 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
CHEMBL7318 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm050247c
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm050247c
11190151 129656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
CHEMBL367832 129656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm050247c
11014674 161391 4 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm050247c
CHEMBL415464 161391 4 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm050247c
44328120 206296 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm050247c
CHEMBL97492 206296 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm050247c
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2010.12.007
134129927 141882 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2c3c(ccc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
CHEMBL3889852 141882 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 352 2 1 4 3.4 O=S(=O)(c1ccccc1)n1ccc2c3c(ccc21)[C@H]1CCNCC[C@@H]31 10.1016/j.bmc.2016.10.010
2726 906 64 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 906 64 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 906 64 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 906 64 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 906 64 None -10 72 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
44425698 85866 6 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 330 6 2 3 3.4 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNC3)cc1 10.1016/j.bmcl.2006.10.036
CHEMBL231326 85866 6 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 330 6 2 3 3.4 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CNC3)cc1 10.1016/j.bmcl.2006.10.036
44425711 86101 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 504 4 1 3 5.6 CN1CCc2cc(Br)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231546 86101 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 504 4 1 3 5.6 CN1CCc2cc(Br)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
44425714 86251 0 None -19 5 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 460 4 1 3 5.5 CN1CCc2cc(Cl)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231648 86251 0 None -19 5 Human 7.3 pKi = 7.3 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 460 4 1 3 5.5 CN1CCc2cc(Cl)c(NS(=O)(=O)c3ccc(-c4ccc(Cl)cc4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
156009804 176478 0 None - 1 Human 6.3 pKi = 6.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 424 4 2 6 3.7 O=S(=O)(Nc1ccc2sc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.ejmech.2018.11.017
CHEMBL4632617 176478 0 None - 1 Human 6.3 pKi = 6.3 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 424 4 2 6 3.7 O=S(=O)(Nc1ccc2sc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.ejmech.2018.11.017
155541676 172490 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4519436 172490 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 5 2 5 3.9 CCC(=O)Nc1nc(C)c(-c2cccc3c2ccn3S(=O)(=O)c2ccccc2)[nH]1 10.1016/j.ejmech.2019.06.001
44568102 183441 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 460 6 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(CCc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL482099 183441 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 460 6 0 5 4.5 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(CCc2ccccc2)CC3)c1 10.1016/j.bmcl.2008.06.030
71458651 81022 0 None -50 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159477 81022 0 None -50 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 439 8 1 5 3.8 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cccc3cccnc23)C1 10.1016/j.ejmech.2012.07.043
57399868 71212 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949978 71212 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963032 71212 0 None -39 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
164610456 183918 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4847379 183918 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 328 5 1 7 1.7 CCC(Oc1ccccc1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
156014787 176971 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640281 176971 0 None -4 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 428 6 1 5 3.6 COc1cc2c3c(c1OCC1CC1)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
4189 205195 91 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
168282454 190621 0 None -63 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 485 11 4 8 3.6 Nc1nc(NCCCCN2CCN(c3ccccc3)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5189648 190621 0 None -63 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 485 11 4 8 3.6 Nc1nc(NCCCCN2CCN(c3ccccc3)CC2)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
3198 203802 73 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -32 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
155531846 171079 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 300 4 1 7 0.8 CN1CCN(c2nc(N)nc(COc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
CHEMBL4465929 171079 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 300 4 1 7 0.8 CN1CCN(c2nc(N)nc(COc3ccccc3)n2)CC1 10.1016/j.ejmech.2019.06.022
155524957 175771 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4455845 175771 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595569 175771 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2019.06.028
68115847 131734 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 5 2 6 3.1 CC(C)(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696969 131734 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 401 5 2 6 3.1 CC(C)(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
44403095 134711 0 None -2818 6 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL372453 134711 0 None -2818 6 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
57392614 70424 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950770 70424 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 nan
162663184 181414 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 596 12 1 7 5.5 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4780498 181414 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 596 12 1 7 5.5 C#CCNC1CCc2c(OCCCCCN3CCN(c4cccc5c4ccn5S(=O)(=O)c4ccccc4)CC3)cccc21 10.1016/j.ejmech.2020.112765
164616670 184030 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4849077 184030 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
57392614 70424 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950770 70424 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 358 2 1 5 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccsc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
16718827 174836 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
CHEMBL457570 174836 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 406 6 1 3 4.9 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2C1 10.1021/jm8009469
11384675 62863 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049615n
CHEMBL179034 62863 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 4.2 O=C1OCc2ccccc2N1C1CCN(S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm049615n
44263956 202743 1 None 2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm990550b
CHEMBL7220 202743 1 None 2 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 0 3 2.3 COc1ccc2c(c1)c(CCN(C)C)cn2C 10.1021/jm990550b
118736375 118442 0 None -19 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 477 6 0 9 2.2 Cc1cccc(N2CCN(CCCCn3c(C)cn4c5c(=O)n(C)c(=O)n(C)c5nc34)CC2)c1C 10.1016/j.ejmech.2015.04.046
CHEMBL3423339 118442 0 None -19 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 477 6 0 9 2.2 Cc1cccc(N2CCN(CCCCn3c(C)cn4c5c(=O)n(C)c(=O)n(C)c5nc34)CC2)c1C 10.1016/j.ejmech.2015.04.046
56593799 65358 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834343 65358 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 360 4 1 5 1.4 CCN/C(=N\S(=O)(=O)c1c(C)nn(C)c1Cl)N1CC(CC)C=N1 10.1021/jm200466r
17055181 161902 2 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 409 7 1 2 6.2 Cc1ccc(COc2ccc(Br)cc2CNC(C)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.010
CHEMBL4166667 161902 2 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 409 7 1 2 6.2 Cc1ccc(COc2ccc(Br)cc2CNC(C)c2ccccc2)cc1 10.1016/j.ejmech.2018.04.010
275 3308 6 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
3246 3308 6 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
5312144 3308 6 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
CHEMBL46071 3308 6 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
71453280 81028 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
CHEMBL2159483 81028 0 None -57 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 458 8 1 4 4.1 O=S(=O)(NC1CCN(CCOc2ccccc2-c2ccccc2)C1)c1cc(F)ccc1F 10.1016/j.ejmech.2012.07.043
13069602 120100 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360996 120100 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546112 120100 0 None -5128 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 430 6 0 8 1.7 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57399548 70409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950754 70409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
58258869 128473 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(N4CCCC4)c31)C1CCC(C2)N1 nan
CHEMBL3669672 128473 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 421 3 1 5 4.0 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(N4CCCC4)c31)C1CCC(C2)N1 nan
12 1524 14 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 1524 14 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 1524 14 None 6 7 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
11849745 79433 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
CHEMBL212178 79433 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm060469q
6761 67457 17 None -9 18 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67457 17 None -9 18 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
137654850 158425 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 341 3 1 5 3.0 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00482
CHEMBL4096141 158425 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 341 3 1 5 3.0 CC1=C(CO)Oc2cccc3c2c1cn3S(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.6b00482
137650191 156649 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4075727 156649 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccc(Cl)cc3)n2)CC1 10.1016/j.ejmech.2017.04.033
156014079 176682 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2ccccc12 10.1016/j.bmc.2020.115459
CHEMBL4636031 176682 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1cccc2ccccc12 10.1016/j.bmc.2020.115459
57399548 70409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950754 70409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 3 1 4 3.8 CCn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11849745 79433 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
CHEMBL212178 79433 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 304 6 1 3 2.6 CN(C)CCc1cccc(NS(=O)(=O)c2ccccc2)c1 10.1021/jm070910s
24783295 176216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2oc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
CHEMBL460626 176216 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1ccc2oc(N3CCNCC3)nc2c1)c1cccc2ccccc12 10.1016/j.bmcl.2008.12.107
118731503 117732 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 555 9 1 6 5.7 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409233 117732 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 555 9 1 6 5.7 O=C1CCc2ccc(OCCCCN3CC=C(c4cn(S(=O)(=O)c5ccccc5)c5ccccc45)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
118731507 117735 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 11 2 6 4.8 O=C1CCc2ccc(OCCCCNCCc3cn(S(=O)(=O)c4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409236 117735 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 11 2 6 4.8 O=C1CCc2ccc(OCCCCNCCc3cn(S(=O)(=O)c4ccccc4)c4ccccc34)cc2N1 10.1016/j.ejmech.2014.12.045
57391618 71125 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71125 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71125 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
11190151 129656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367832 129656 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2ccn(CCN3CCCC3)c2c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
56944086 111590 0 None -999 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 420 8 1 7 2.8 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289976 111590 0 None -999 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 420 8 1 7 2.8 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cccs1 10.1021/jm401895u
4601 205020 29 None -2 17 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL1201023 205020 29 None -2 17 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
CHEMBL900 205020 29 None -2 17 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 nan
155525596 170492 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 2 4 4.9 Oc1ccc(-c2ccc(CNCCc3coc4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4457045 170492 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 351 6 2 4 4.9 Oc1ccc(-c2ccc(CNCCc3coc4ccc(F)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
68109040 131156 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 2.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNC(CO)C3 nan
CHEMBL3692897 131156 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 377 3 2 5 2.9 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNC(CO)C3 nan
49781471 17579 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 533 8 2 8 4.3 COc1ccc(NS(=O)(=O)c2ccc(-c3ncc(-c4ccc(N(C)C)cc4)o3)cc2)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1258714 17579 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 533 8 2 8 4.3 COc1ccc(NS(=O)(=O)c2ccc(-c3ncc(-c4ccc(N(C)C)cc4)o3)cc2)cc1N1CCNCC1 10.1021/jm1007177
8431 1456 6 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
9843179 1456 6 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
CHEMBL69257 1456 6 None -234 5 Human 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptorCompound was evaluated for its ability to displace [3H]LSD binding from human recombinant 5-hydroxytryptamine 6 receptor
ChEMBL 386 6 1 2 5.2 O=C1Nc2c3C1(CCCCN1CCC(=CC1)c1ccccc1)CCCc3ccc2 10.1021/jm980519u
162657889 180475 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCN(CC(F)(F)F)CC3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4759633 180475 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 423 4 0 5 3.6 O=S(=O)(c1ccccc1)n1ccc2cc(N3CCN(CC(F)(F)F)CC3)ccc21 10.1016/j.ejmech.2020.112916
155534301 171369 0 None -123 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 415 8 0 5 4.0 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4470304 171369 0 None -123 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 415 8 0 5 4.0 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2019.06.029
156009734 176592 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 393 5 2 4 3.7 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4634426 176592 0 None -1 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 393 5 2 4 3.7 COc1cc2c3c(c1OCC1CC1)-c1cc(NC(N)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
155555200 173791 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.2 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
CHEMBL4551512 173791 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 396 4 0 3 4.2 O=S(=O)(c1ccccc1)N1CCc2ccc(C3CCN(C4CCC4)CC3)cc21 10.1016/j.bmcl.2016.07.055
145975992 162964 0 None -20 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 393 4 1 3 3.6 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4202520 162964 0 None -20 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 393 4 1 3 3.6 O=C1Nc2ccccc2C12CCN(CCN1CCC(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
142601329 185935 3 None -79 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 185935 3 None -79 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
16118924 59835 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642855 59835 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739686 59835 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCNCC3)ccc12 10.1016/j.bmc.2010.10.033
164619932 185625 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 386 8 1 3 4.3 Cc1cccc(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4873096 185625 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 386 8 1 3 4.3 Cc1cccc(CNCCOc2cccc3c2CC(=O)N3Cc2ccccc2)c1 10.1016/j.ejmech.2021.113792
16718917 181100 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
CHEMBL477650 181100 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 412 6 1 4 5.0 CC1=C(CCN(C)C)c2cc(NS(=O)(=O)c3csc4ccccc34)ccc2C1 10.1021/jm8009469
66801140 111171 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
CHEMBL3286432 111171 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 482 8 1 6 4.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(F)c(Cl)c1 10.1021/jm401895u
68108927 131126 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
CHEMBL3692868 131126 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 407 2 1 4 4.6 O=S(=O)(c1cccc(C(F)(F)F)c1)c1ccc2oc3c(c2c1)C1CCC(C3)N1 nan
24966736 83612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207377 83612 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 403 4 0 5 3.3 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2012.10.057
11014674 161391 4 None - 1 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm021085c
CHEMBL415464 161391 4 None - 1 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 390 2 1 4 3.0 Nc1ccc(S(=O)(=O)c2cc(Br)nc(Br)c2)cc1 10.1021/jm021085c
4407909 192264 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192264 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192264 1 None -9 10 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
1530 2151 44 None -58 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -58 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -58 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -58 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -58 20 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
155557890 174133 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 333 6 3 4 3.9 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4559790 174133 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 333 6 3 4 3.9 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ncccc34)o2)cc1 10.1016/j.ejmech.2019.111857
68109274 131137 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
CHEMBL3692878 131137 0 None - 1 Human 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 357 2 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CC1CCC3N1 nan
156013203 176908 0 None -16 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
CHEMBL4639203 176908 0 None -16 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 477 8 0 4 4.7 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2020.115459
71449645 81035 0 None -21 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
CHEMBL2159490 81035 0 None -21 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 428 8 1 5 4.0 CC(C)c1ccccc1OCCN1CC[C@H](NS(=O)(=O)c2ccc(Cl)s2)C1 10.1016/j.ejmech.2012.07.043
127025242 137277 0 None -269 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2cccc(F)c2)C3)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759617 137277 0 None -269 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2cccc(F)c2)C3)c1 10.1016/j.ejmech.2015.11.040
44390095 11640 15 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1181566 11640 15 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL180298 11640 15 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 290 1 1 2 3.0 Brc1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44388986 64443 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 438 3 0 5 4.9 CC(C)(C)OC(=O)N1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL181938 64443 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 438 3 0 5 4.9 CC(C)(C)OC(=O)N1CC=C(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
9796627 96205 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 96205 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
6918515 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 2574 33 None 4 6 Human 7.3 pKi = 7.3 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
162660390 180648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 570 12 0 7 4.9 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
CHEMBL4761469 180648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 570 12 0 7 4.9 C#CCN(C)Cc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2020.112765
57397900 70408 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 338 2 2 3 3.4 O=S(=O)(c1ccccc1)c1ccc2[nH]c3c(c2c1)C1CCC(C3)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950753 70408 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 338 2 2 3 3.4 O=S(=O)(c1ccccc1)c1ccc2[nH]c3c(c2c1)C1CCC(C3)N1 10.1016/j.bmcl.2012.01.022
127045873 139494 0 None 22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 438 3 0 6 3.3 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(C)(=O)=O)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3800153 139494 0 None 22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 438 3 0 6 3.3 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(C)(=O)=O)c3n2)CC1 10.1016/j.bmcl.2016.04.024
24784069 190511 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1cccc(F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518781 190511 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1cccc(F)c1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
90656153 110335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
CHEMBL3260785 110335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 306 2 1 2 2.9 O=C1CC(c2ccccc2)CN1c1ccc2c(c1)CCNCC2 10.1016/j.bmcl.2014.03.049
66800916 111575 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 518 8 1 7 4.8 Cc1c(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
CHEMBL3289962 111575 0 None -11 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 518 8 1 7 4.8 Cc1c(S(=O)(=O)NCCCCN2CCN(c3nsc4ccccc34)CC2)sc2ccc(F)cc12 10.1021/jm401895u
45378934 199961 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL605971 199961 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 406 3 1 6 3.1 Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
11638332 94483 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 319 1 1 2 4.1 CC1(c2ccccc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL254298 94483 1 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 319 1 1 2 4.1 CC1(c2ccccc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human 5HT6RBinding affinity to human 5HT6R
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.ejmech.2017.04.033
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligandBinding constant towards serotonin receptor subtype 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD as radioligand
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm021085c
CHEMBL5076882 212695 0 None -14 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cccc(Cl)c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm5003952
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1021/jm030030n
44328120 206296 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm030030n
CHEMBL97492 206296 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 3 3 5 1.8 Nc1ccc(S(=O)(=O)Nc2cc(N)nc(Br)c2)cc1 10.1021/jm030030n
135 2496 38 None -21 57 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
1796 2496 38 None -21 57 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
4184 2496 38 None -21 57 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
CHEMBL6437 2496 38 None -21 57 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
DB06148 2496 38 None -21 57 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm030030n
155511262 168977 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cccc(O)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4435528 168977 0 None -1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 362 7 3 4 4.5 COc1ccc2[nH]cc(CCNCc3ccc(-c4cccc(O)c4)o3)c2c1 10.1016/j.ejmech.2019.111857
164625686 185737 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 3.9 O=C1Cc2c(OCCNCc3ccccc3)cccc2N1Cc1ccccc1 10.1016/j.ejmech.2021.113792
CHEMBL4874675 185737 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 372 8 1 3 3.9 O=C1Cc2c(OCCNCc3ccccc3)cccc2N1Cc1ccccc1 10.1016/j.ejmech.2021.113792
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2009.04.108
24763350 62292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 355 3 1 4 3.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccccc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783599 62292 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 355 3 1 4 3.2 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccccc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
274 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
5312145 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
CHEMBL433461 3287 39 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1016/j.bmcl.2007.11.045
90656163 110345 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(N3CCNCC3)ccnc2c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260796 110345 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 372 3 1 4 3.2 O=C1CC(c2ccccc2)CN1c1ccc2c(N3CCNCC3)ccnc2c1 10.1016/j.bmcl.2014.03.049
57396813 71201 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949930 71201 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963007 71201 0 None -5 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from rat recombinant 5HT6 receptorDisplacement of [3H]LSD from rat recombinant 5HT6 receptor
ChEMBL 403 5 1 6 3.2 COc1cc(OC(C)C)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
68115734 131736 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 3 2 5 3.1 CC(C)(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696971 131736 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 371 3 2 5 3.1 CC(C)(O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
11475760 119992 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm049615n
CHEMBL354418 119992 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 423 6 1 7 3.4 CN(C)CCn1ccc2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1021/jm049615n
23652922 56403 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 431 4 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2010.11.001
CHEMBL1642428 56403 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 431 4 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(N3CCN(C)CC3)c3ccc(Cl)cc32)cc1 10.1016/j.bmcl.2010.11.001
137653132 158360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 401 4 0 5 3.1 Cc1c(CN2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4095446 158360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 401 4 0 5 3.1 Cc1c(CN2CCN(C)CC2)c2ccccc2n1S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
44397117 12913 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1189862 12913 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL539587 12913 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
155512944 169152 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 249 1 1 2 3.4 Cn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4438349 169152 0 None -11 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 249 1 1 2 3.4 Cn1cncc1-c1c[nH]c2ccc(Cl)c(F)c12 10.1016/j.ejmech.2019.03.017
71453282 81036 0 None -69 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159491 81036 0 None -69 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 462 8 1 5 4.5 O=S(=O)(N[C@H]1CCN(CCOc2ccccc2-c2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
49781254 17004 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 772 16 2 9 6.6 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
CHEMBL1256258 17004 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 772 16 2 9 6.6 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCN(CCCCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)CC1 10.1021/jm1007177
71574298 85858 0 None -13 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 526 8 1 5 5.1 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312936 85858 0 None -13 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 526 8 1 5 5.1 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
145976408 163326 0 None -83 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 424 5 1 4 3.4 O=C1Nc2ccccc2C12CCN(CCCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4206881 163326 0 None -83 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 424 5 1 4 3.4 O=C1Nc2ccccc2C12CCN(CCCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
155532887 171242 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 7 1 4 4.8 COc1cccc(-c2ccc(CNCCc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4468235 171242 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 360 7 1 4 4.8 COc1cccc(-c2ccc(CNCCc3cn(C)c4ccccc34)o2)c1 10.1016/j.ejmech.2019.111857
155543192 172716 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4525628 172716 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2ccc3c(c2)CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
134949378 180908 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccccc3)ccc21 10.1016/j.ejmech.2020.112916
CHEMBL4764769 180908 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 333 3 0 3 4.5 O=S(=O)(c1ccccc1)n1ccc2cc(-c3ccccc3)ccc21 10.1016/j.ejmech.2020.112916
127025243 137218 0 None -562 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
CHEMBL3759205 137218 0 None -562 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 446 8 1 4 4.3 CC(C)c1cccc(OCCN2C3CCC2CC(NS(=O)(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.11.040
137649536 156759 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4077077 156759 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 318 3 1 6 1.5 CN1CCN(c2nc(N)nc(Cc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2017.04.033
126720443 162414 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 5 1 5 2.8 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4174854 162414 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 5 1 5 2.8 CCc1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
45487113 196075 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 371 6 0 6 2.6 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccccc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
CHEMBL571635 196075 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 371 6 0 6 2.6 CC(=O)c1ccc2c(n1)c(S(=O)(=O)c1ccccc1)cn2CCN(C)C 10.1016/j.bmcl.2009.10.067
57391569 71181 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1949929 71181 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
CHEMBL1962864 71181 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1F 10.1016/j.bmcl.2011.12.026
66801335 111561 0 None -5 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 8 1 7 3.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
CHEMBL3289948 111561 0 None -5 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 500 8 1 7 3.7 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(OC(F)(F)F)cc1 10.1021/jm401895u
68108832 131153 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
CHEMBL3692894 131153 0 None - 1 Human 7.3 pKi = 7.3 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 361 2 1 4 4.1 CC1NCCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c21 nan
90644078 111597 0 None -18 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 490 7 1 7 4.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
CHEMBL3289983 111597 0 None -18 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 490 7 1 7 4.2 O=S(=O)(NCCCN1CCN(c2noc3ccccc23)CC1)c1cc2ccc(Cl)cc2s1 10.1021/jm401895u
2880253 162157 9 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
CHEMBL4170813 162157 9 None 1 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 351 7 1 2 5.4 CCC1(C)CC(CCNCc2ccccc2)(c2ccc(C)cc2)CCO1 10.1016/j.ejmech.2018.04.010
134155476 150693 0 None -53 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
CHEMBL3960056 150693 0 None -53 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 455 10 1 3 5.9 C[C@@H](NC(=O)CCCCCN1CCN(c2ccccc2-c2ccccc2)CC1)c1ccccc1 10.1016/j.ejmech.2016.05.005
57391620 71221 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949769 71221 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963098 71221 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 389 6 1 6 2.4 COCCOc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
5640104 117436 11 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 429 4 1 5 3.4 NC(=O)C1CCN(c2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2015.03.049
CHEMBL3403342 117436 11 None -1 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 429 4 1 5 3.4 NC(=O)C1CCN(c2c(S(=O)(=O)c3ccccc3)cnc3ccc(Cl)cc23)CC1 10.1016/j.bmcl.2015.03.049
156012551 176763 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 8 0 5 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
CHEMBL4637294 176763 0 None -15 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 470 8 0 5 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.bmc.2020.115459
44390011 12146 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1184633 12146 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL360663 12146 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 316 3 1 3 3.5 O=C(c1ccccc1)c1ccc(N2CCNCC2)c2ccccc12 10.1016/j.bmcl.2005.01.031
44401434 165796 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 275 4 0 1 4.6 CN(C)CCC1=C/C(=C\c2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
CHEMBL427354 165796 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 275 4 0 1 4.6 CN(C)CCC1=C/C(=C\c2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.02.070
44395604 66392 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)c2cn(CCN(C)C)c3ccccc23)cc1 10.1016/j.bmcl.2004.09.003
CHEMBL185672 66392 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 342 5 0 4 3.3 Cc1ccc(S(=O)(=O)c2cn(CCN(C)C)c3ccccc23)cc1 10.1016/j.bmcl.2004.09.003
16118925 59836 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642856 59836 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739694 59836 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cc(NC3CCCNC3)ccc12 10.1016/j.bmc.2010.10.033
156019543 177362 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2020.115459
CHEMBL4645525 177362 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 508 10 1 6 5.1 O=S(=O)(NCCCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1016/j.bmc.2020.115459
126720426 162257 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cc(F)ccc1F 10.1016/j.ejmech.2017.12.053
CHEMBL4172424 162257 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 357 4 1 5 2.7 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cc(F)ccc1F 10.1016/j.ejmech.2017.12.053
118731511 117745 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 9 1 6 4.6 NC(=O)c1ccccc1OCCCN1CCC(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409246 117745 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 517 9 1 6 4.6 NC(=O)c1ccccc1OCCCN1CCC(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
11750876 200112 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
CHEMBL606870 200112 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 433 5 3 3 4.0 O=S(=O)(Nc1ccc2[nH]cc(C[C@@H]3CCCN3)c2c1)c1ccc(Br)cc1 10.1021/jm049243i
11234781 119915 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
CHEMBL353739 119915 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc21 10.1021/jm049615n
44387804 130860 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 5.5 Cc1c(S(=O)(=O)Nc2cccc3c2cc(C)n3CCN(C)C)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL368973 130860 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 5.5 Cc1c(S(=O)(=O)Nc2cccc3c2cc(C)n3CCN(C)C)sc2ccc(Cl)cc12 10.1021/jm049615n
2816054 110334 20 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 1 1 3 2.6 O=C1CSC2(C(=O)Nc3ccccc32)N1c1ccccc1 10.1016/j.bmcl.2014.03.049
CHEMBL3260784 110334 20 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 296 1 1 3 2.6 O=C1CSC2(C(=O)Nc3ccccc32)N1c1ccccc1 10.1016/j.bmcl.2014.03.049
155534575 171380 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 429 8 0 7 2.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4470487 171380 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 429 8 0 7 2.0 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
68109126 131140 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCCC3 nan
CHEMBL3692881 131140 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 1 4 3.3 O=S(=O)(c1ccccc1)c1ccc2oc3c(c2c1)CNCCC3 nan
242 467 117 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
34 467 117 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
60795 467 117 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
CHEMBL1112 467 117 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
DB01238 467 117 None -144 51 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2010.07.105
168277374 189775 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 441 8 4 6 4.6 Nc1nc(NCCc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5177186 189775 0 None -9 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 441 8 4 6 4.6 Nc1nc(NCCc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
6090 34344 17 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.08.068
CHEMBL142936 34344 17 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2006.08.068
164615340 184847 0 None 3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4861431 184847 0 None 3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
155518974 169782 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)cc1 10.1016/j.bmcl.2019.06.029
CHEMBL4447330 169782 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccc(N2CCN(CCCCCCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)cc1 10.1016/j.bmcl.2019.06.029
274 3287 39 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
5312145 3287 39 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
CHEMBL433461 3287 39 None -1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 10.1007/s00044-004-0121-8
155556168 173855 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 365 5 1 7 2.0 COc1ccc(Cc2nc(N3CCNCC3)nc3cccnc23)c(OC)c1 10.1016/j.ejmech.2019.111857
CHEMBL4552950 173855 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 365 5 1 7 2.0 COc1ccc(Cc2nc(N3CCNCC3)nc3cccnc23)c(OC)c1 10.1016/j.ejmech.2019.111857
137645440 157454 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4085349 157454 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3cccc(F)c3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
44403091 139827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 357 3 1 6 2.9 Cc1nc(C)c(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)o1 10.1016/j.bmcl.2005.07.028
CHEMBL380777 139827 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 357 3 1 6 2.9 Cc1nc(C)c(S(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)o1 10.1016/j.bmcl.2005.07.028
45488131 196904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
CHEMBL578411 196904 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 292 3 2 3 2.6 c1ccc(Cc2nc3c(N4CCNCC4)cccc3[nH]2)cc1 10.1021/jm901672k
9945214 81605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counterDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counter
ChEMBL 326 2 2 3 2.8 NC1CCc2[nH]c3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165521 81605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counterDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells after 1 hr by scintillation counter
ChEMBL 326 2 2 3 2.8 NC1CCc2[nH]c3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 10.1016/j.bmcl.2012.06.002
11589069 95800 0 None -354 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 95800 0 None -354 8 Human 6.2 pKi = 6.2 Binding
Inhibition of 5HT6 receptorInhibition of 5HT6 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
2867758 161493 7 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 339 6 1 2 5.5 Cc1ccc(C(C)(C)CC(C)NCc2ccc(C(F)(F)F)cc2)o1 10.1016/j.ejmech.2018.04.010
CHEMBL4160177 161493 7 None 1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 339 6 1 2 5.5 Cc1ccc(C(C)(C)CC(C)NCc2ccc(C(F)(F)F)cc2)o1 10.1016/j.ejmech.2018.04.010
118729733 117431 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 394 4 1 3 5.4 O=S(=O)(Nc1ccccc1-c1nccc2ccccc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403338 117431 0 None -1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 394 4 1 3 5.4 O=S(=O)(Nc1ccccc1-c1nccc2ccccc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2015.03.049
58258846 128470 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 453 5 1 6 2.8 CN(C)C(=O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669669 128470 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 453 5 1 6 2.8 CN(C)C(=O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
168277502 190121 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 468 8 0 5 6.2 S=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
CHEMBL5182383 190121 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 468 8 0 5 6.2 S=c1n(CCCCCCN2CCN(c3cccc(Cl)c3)CC2)c2cccc3c2n1CCC3 10.1016/j.ejmech.2022.114319
2812 4711 96 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -36 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
23906630 117426 4 None 2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 1 2 2.9 O=S(=O)(c1ccc(F)cc1)N1CC=c2ccccc2=C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL3403333 117426 4 None 2 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 404 3 1 2 2.9 O=S(=O)(c1ccc(F)cc1)N1CC=c2ccccc2=C1c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
168273001 189618 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 403 9 4 7 3.3 COc1ccccc1CCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5174637 189618 0 None -3 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 403 9 4 7 3.3 COc1ccccc1CCNc1nc(N)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
155549153 173662 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 420 3 0 6 3.4 CC(=O)N1CCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4548837 173662 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 420 3 0 6 3.4 CC(=O)N1CCn2c1nc(C)c2-c1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2019.06.001
155563286 174755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cc(F)ccc12 10.1016/j.ejmech.2019.03.017
CHEMBL4573883 174755 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cc(F)ccc12 10.1016/j.ejmech.2019.03.017
11695841 113675 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 5 2 3 3.7 N=C(N)CCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1021/jm5003952
CHEMBL3329444 113675 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 342 5 2 3 3.7 N=C(N)CCC1CCCc2cc(S(=O)(=O)c3ccccc3)ccc21 10.1021/jm5003952
4494260 154112 15 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 360 5 1 5 3.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(Cl)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL399478 154112 15 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 360 5 1 5 3.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccc(Cl)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
137656602 159054 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103190 159054 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3cc(Cl)ccc23)CC1 10.1021/acs.jmedchem.6b01662
44438689 148286 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 5 0 4 2.3 CC(C)S(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
CHEMBL394097 148286 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 294 5 0 4 2.3 CC(C)S(=O)(=O)n1cc(CCN(C)C)c2ccccc21 10.1016/j.bmcl.2006.12.089
57395598 68083 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
CHEMBL1917346 68083 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 395 7 1 4 3.4 O=S(=O)(NCCCCN1CCc2ccccc2C1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.09.044
156018601 177320 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 414 6 1 5 3.4 C=CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4644833 177320 0 None -14 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 414 6 1 5 3.4 C=CCOc1c(OC)cc2c3c1-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
118731508 117742 0 None -19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 465 9 1 4 5.3 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409243 117742 0 None -19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 465 9 1 4 5.3 NC(=O)c1ccccc1OCCCN1CC=C(c2cn(Cc3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2014.12.045
118464427 137806 0 None -213 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 137806 0 None -213 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
71727069 101932 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL2401935 101932 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
CHEMBL3039672 101932 0 None -50 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 4 0 5 4.3 COc1ccccc1N1CCN(Cc2ccc3oc4ccccc4c(=O)c3c2)CC1 10.1016/j.bmcl.2013.05.062
155560272 174514 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 476 4 1 5 3.6 CC1=CC=CN2C(=O)C3C=C(S(=O)(=O)c4ccccc4)C(=N)N(Cc4ccc(F)cc4)C3N=C12 10.1016/j.ejmech.2019.111857
CHEMBL4568668 174514 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 476 4 1 5 3.6 CC1=CC=CN2C(=O)C3C=C(S(=O)(=O)c4ccccc4)C(=N)N(Cc4ccc(F)cc4)C3N=C12 10.1016/j.ejmech.2019.111857
118731351 117685 0 None -30 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409035 117685 0 None -30 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 8 1 4 4.1 NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)CCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1016/j.ejmech.2014.12.041
122483292 137583 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 137583 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 137583 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
155533704 171293 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 383 2 2 2 3.8 CN1C=C2C(NC(=S)NC2c2ccc(F)cc2)/C(=C\c2ccc(F)cc2)C1 10.1016/j.ejmech.2019.111857
CHEMBL4469065 171293 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 383 2 2 2 3.8 CN1C=C2C(NC(=S)NC2c2ccc(F)cc2)/C(=C\c2ccc(F)cc2)C1 10.1016/j.ejmech.2019.111857
2737389 187003 23 None -426 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 187003 23 None -426 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
71574304 85838 0 None -22 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2cccnc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312638 85838 0 None -22 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2cccnc12 10.1016/j.ejmech.2012.11.042
448537 159703 86 None -35 25 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -35 25 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44397102 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.05.076
CHEMBL188144 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2004.05.076
23757269 113954 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.bmcl.2004.05.076
CHEMBL333373 113954 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 receptorBinding affinity against 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/j.bmcl.2004.05.076
44397102 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL188144 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.05.092
44397102 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
CHEMBL188144 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.02.070
126720440 162476 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
CHEMBL4175829 162476 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6R (unknown origin)Binding affinity to 5HT6R (unknown origin)
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1021/acs.jmedchem.0c02009
44397102 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL188144 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
155525318 170421 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
CHEMBL4456224 170421 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cc2ccccc2cn1 10.1021/acsmedchemlett.6b00056
164618100 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4860275 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
164620748 185663 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
CHEMBL4873623 185663 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2022.114645
67156504 161601 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.1c00224
CHEMBL4161904 161601 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 342 3 1 6 1.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCNCC3)nccc21 10.1021/acs.jmedchem.1c00224
126720440 162476 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4175829 162476 0 None 72 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 339 4 1 5 2.6 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(F)c1 10.1016/j.ejmech.2017.12.053
134130413 141702 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 579 8 1 7 5.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884618 141702 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 579 8 1 7 5.9 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
9979009 158549 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4097459 158549 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 5 0 5 3.7 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
10317027 160515 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4062687 160515 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4116630 160515 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 369 4 0 5 2.6 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2010.07.105
164618100 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
164620748 185663 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873623 185663 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
46880757 5951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1080381 5951 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 390 3 0 4 4.5 CN1CCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
46880486 6093 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1081095 6093 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 358 3 1 4 3.5 O=S(=O)(c1cccc(F)c1)c1cn(C2CCCNC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
164612180 184158 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4850764 184158 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 449 9 1 6 4.1 CN(C)c1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
164611496 184875 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 563 8 1 7 5.6 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)C1 10.1016/j.ejmech.2021.113792
CHEMBL4861756 184875 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 563 8 1 7 5.6 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2cccc3ccccc23)C1 10.1016/j.ejmech.2021.113792
164623148 184967 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 424 8 1 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4863101 184967 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 424 8 1 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCc3ccc(F)cc3)cccc21 10.1016/j.ejmech.2021.113792
44397102 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1021/jm8009469
CHEMBL188144 66933 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 278 5 0 2 3.8 CN(C)CCc1cn(Cc2ccccc2)c2ccccc12 10.1021/jm8009469
23655289 88261 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
CHEMBL235986 88261 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 334 4 1 4 3.0 NCCc1cn(S(=O)(=O)c2cccc(Cl)c2)c2ccccc12 10.1021/jm070521y
23655468 88961 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236989 88961 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/jm070521y
127045874 139315 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 4 0 6 4.1 CC(C)S(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3799120 139315 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 466 4 0 6 4.1 CC(C)S(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
23655468 88961 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/acs.jmedchem.5b00179
CHEMBL236989 88961 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counterDisplacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor expressed in HeLa cells after 120 mins by scintillation counter
ChEMBL 340 4 1 5 3.1 NCCc1cn(S(=O)(=O)c2ccc(Cl)s2)c2ccccc12 10.1021/acs.jmedchem.5b00179
57414664 131198 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.9 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692939 131198 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.9 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
164618100 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4860275 184778 0 None 5 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5-HT6 receptor expressed in HEK293 cellsBinding affinity to human 5-HT6 receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 3.0 CCC(Oc1cc(Cl)ccc1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
135398737 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
38 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
722 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
CHEMBL42 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
DB00363 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
58158749 138466 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785512 138466 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 384 3 2 4 2.6 CCN/C(=N\S(=O)(=O)c1cc(O)cc(Cl)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
135398737 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
38 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
722 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
CHEMBL42 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
DB00363 944 89 None -4 91 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2013.12.024
44435646 145027 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL391517 145027 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
68115646 131220 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1C(F)(F)F nan
CHEMBL3692961 131220 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 415 2 1 4 4.6 O=S(=O)(c1cc(Cl)c2oc3c(c2c1)CNCC3)c1ccccc1C(F)(F)F nan
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
44435646 145027 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL391517 145027 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 409 3 1 5 4.1 O=S(=O)(c1cc(Cl)cc(Cl)c1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
23757269 113954 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
CHEMBL333373 113954 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 386 8 0 5 3.8 CCN(CC)CCc1cn(S(=O)(=O)c2ccccc2)c2ccc(OC)cc12 10.1016/s0960-894x(03)00612-7
66801158 111592 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289978 111592 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 464 8 1 6 3.9 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
57414394 131101 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
CHEMBL3692843 131101 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 347 2 1 4 3.6 O=S(=O)(c1cccc(Cl)c1)c1ccc2oc3c(c2c1)CNCC3 nan
52913228 70419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950764 70419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 nan
16117278 59833 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642884 59833 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739659 59833 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1ccc(F)cc1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
52913228 70419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950764 70419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 367 2 2 5 2.9 Cn1c2c(c3cc(S(=O)(=O)c4cccc(N)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
1621 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
17 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
5761 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
CHEMBL263881 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
DB04829 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cellsBinding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm0341204
9849116 205849 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2c(Cl)cc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL94930 205849 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2c(Cl)cc(Cl)cc12 10.1016/s0960-894x(01)00558-3
44398577 132943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 301 3 2 5 1.9 NCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
CHEMBL370672 132943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 301 3 2 5 1.9 NCc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm050247c
46890323 6829 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 402 4 1 4 2.5 O=C1CN(C[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)CCN1 10.1016/j.bmcl.2010.03.110
CHEMBL1084335 6829 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 402 4 1 4 2.5 O=C1CN(C[C@@H]2CCCc3cc(S(=O)(=O)c4cccc(F)c4)ccc32)CCN1 10.1016/j.bmcl.2010.03.110
10295001 134694 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL372287 134694 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 409 3 1 5 3.6 O=S(=O)(c1ccc(Cl)cc1)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
44425704 85519 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 412 4 1 4 4.6 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccc4c(c3)CCN(C)CC4)cc2)s1 10.1016/j.bmcl.2006.10.036
CHEMBL230070 85519 0 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 412 4 1 4 4.6 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccc4c(c3)CCN(C)CC4)cc2)s1 10.1016/j.bmcl.2006.10.036
129103322 166819 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
CHEMBL4294799 166819 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation countingDisplacement of [3H]-lysergic acid diethylamide from human serotonin 5-HT6 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting
ChEMBL 463 6 1 5 4.5 O=C1CCc2cc(C(O)CCCN3CCC(c4noc5cc(F)ccc45)CC3)cc3c2N1CC3 10.1021/acs.jmedchem.8b01096
66803474 155775 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4065568 155775 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 429 6 2 3 4.2 Cc1cccc(S(=O)(=O)NCCN2CC=C(c3c[nH]c4ccc(Cl)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
118654428 191161 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5197660 191161 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 405 4 1 5 3.5 Cc1ccc(S(=O)(=O)n2cc(C(F)F)c3c(N4CCNCC4)cccc32)cc1 10.1016/j.bmc.2022.116950
56593931 65361 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
CHEMBL1834347 65361 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 368 3 1 3 2.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCCC2 10.1021/jm200466r
25263338 183586 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 344 5 1 3 5.0 CCC(Oc1nccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL482988 183586 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 344 5 1 3 5.0 CCC(Oc1nccc(C2CCNCC2)c1C)c1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
67085495 127391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 3.4 CNc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664737 127391 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 381 3 2 5 3.4 CNc1cccc(S(=O)(=O)c2ccc3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
3028929 206419 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 6 0 3 3.8 COc1ccc2c(c1)c(CCN(C)C)cn2Cc1ccccc1 10.1021/jm030030n
CHEMBL98237 206419 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 308 6 0 3 3.8 COc1ccc2c(c1)c(CCN(C)C)cn2Cc1ccccc1 10.1021/jm030030n
53327611 69411 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935601 69411 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 401 2 1 5 3.6 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)C1(CCCOC1)NCC3 10.1016/j.bmcl.2011.11.050
164624187 185264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
CHEMBL4867606 185264 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 464 9 1 7 4.0 CC(=O)Oc1cccc(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2021.113792
25263343 183568 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(COc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482938 183568 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 299 4 1 2 4.2 Cc1c(COc2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
56944383 111627 0 None -9 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 111627 0 None -9 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
57414388 131098 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692840 131098 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 2 0 4 3.3 CN1CCc2oc3ccc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
16071727 59786 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642848 59786 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739253 59786 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 366 5 3 5 2.9 NCCNc1ccc2[nH]nc(S(=O)(=O)c3cccc4ccccc34)c2c1 10.1016/j.bmc.2010.10.033
16117154 59831 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642881 59831 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739657 59831 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 374 4 3 5 2.7 O=S(=O)(c1cccc(F)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
137651613 156630 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 6 0 6 3.8 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4075502 156630 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 491 6 0 6 3.8 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3Br)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
10275386 63581 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 445 5 2 3 5.4 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(-c5ccccc5)cc4)cc23)CC1 10.1021/jm049615n
CHEMBL180582 63581 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 445 5 2 3 5.4 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4ccc(-c5ccccc5)cc4)cc23)CC1 10.1021/jm049615n
16223064 81647 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 430 5 0 6 4.0 COc1ccc(S(=O)(=O)n2c3c(c4cc(SC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165562 81647 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 430 5 0 6 4.0 COc1ccc(S(=O)(=O)n2c3c(c4cc(SC)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
67085507 127414 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 450 3 1 5 4.6 Cc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664760 127414 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 450 3 1 5 4.6 Cc1cc(S(=O)(=O)c2cccc(OC(F)(F)F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
1621 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2396 16 None -16 44 Human 8.2 pKi = 8.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5113605 79313 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1021/jm060469q
CHEMBL211577 79313 3 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 302 3 1 4 1.9 O=S(=O)(c1ccccc1)c1ccc(N2CCNCC2)cc1 10.1021/jm060469q
44327999 111909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
44327999 111909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
CHEMBL329739 111909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL329739 111909 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 329 4 1 5 2.5 CN(C)Cc1cn(S(=O)(=O)c2ccc(N)cc2)c2ccccc12 10.1021/jm030030n
21071390 1956 48 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
8689 1956 48 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
CHEMBL3286580 1956 48 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
DB11957 1956 48 None -2 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 minsDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
ChEMBL 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 10.1016/j.ejmech.2020.113059
137630883 160577 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4073450 160577 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4117188 160577 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 5 1 6 2.4 COc1ccc2c(c1)c(CN1CCNCC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
57396970 69400 0 None -4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935590 69400 0 None -4 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 331 2 1 4 3.1 O=S(=O)(c1cccc(F)c1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
71151929 117762 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 0 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409263 117762 0 None 6 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 507 9 0 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCOc4ccc(F)cc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
25263320 188258 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL506736 188258 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 313 4 1 2 4.7 Cc1c(O[C@@H](C)c2cccc(F)c2)cccc1C1CCNCC1 10.1016/j.bmcl.2009.03.077
52912975 70413 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950758 70413 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 nan
15480742 12914 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL1189863 12914 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
CHEMBL539589 12914 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 200 2 2 1 2.5 c1ccc2c(C[C@H]3CCCN3)c[nH]c2c1 10.1016/j.bmcl.2005.05.092
49756 202609 9 None 2 8 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL7143 202609 9 None 2 8 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm030030n
44476704 81931 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
CHEMBL2172182 81931 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 nan
49756 202609 9 None 2 8 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 202609 9 None 2 8 Human 7.2 pKi = 7.2 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
137635884 155359 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 427 7 2 3 4.1 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
CHEMBL4060649 155359 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 427 7 2 3 4.1 Cc1cccc(S(=O)(=O)NCCCN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)c1 10.1021/acs.jmedchem.7b00839
118626140 165365 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250244 165365 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
155515318 169417 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 3 3 5.1 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(Cl)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4442111 169417 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 366 6 3 3 5.1 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(Cl)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
2726 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
52912975 70413 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950758 70413 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 370 2 1 4 3.5 Cn1c2c(c3cc(S(=O)(=O)c4ccc(F)cc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
10274390 184215 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 431 5 0 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(Cc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4851655 184215 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 431 5 0 5 4.2 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(Cc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2021.113792
155555224 173777 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4551220 173777 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 371 4 0 4 2.6 CCN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
68115743 131743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1ccc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)n1 nan
CHEMBL3696978 131743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 3 1 6 3.3 Cn1ccc(-c2cc(S(=O)(=O)c3ccccc3)cc3c4c(oc23)CCNC4)n1 nan
2726 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 906 64 None -10 72 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]LSD from 5-HT6 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
44476704 81931 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172182 81931 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 342 2 0 6 1.9 Cc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
44386815 61443 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 2 1 4 3.8 COc1ccc2c(c1)c1c(n2C(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
CHEMBL177233 61443 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 320 2 1 4 3.8 COc1ccc2c(c1)c1c(n2C(=O)c2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
44386665 130825 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 306 3 1 3 4.2 COc1ccc2c(c1)c1c(n2Cc2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
CHEMBL368783 130825 0 None - 1 Human 5.2 pKi = 5.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 306 3 1 3 4.2 COc1ccc2c(c1)c1c(n2Cc2ccc(N)cc2)CCCC1 10.1016/j.bmcl.2004.01.071
1353 1880 85 None -1047 85 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 1880 85 None -1047 85 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 1880 85 None -1047 85 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 1880 85 None -1047 85 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 1880 85 None -1047 85 Human 5.2 pKi = 5.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
44438743 150851 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 2 1 2 4.2 Nc1ccc(Cn2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL396149 150851 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 2 1 2 4.2 Nc1ccc(Cn2c3c(c4ccccc42)CCCC3)cc1 10.1016/j.bmcl.2006.12.089
155540147 172359 0 None 14 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 233 1 1 2 2.8 Cn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4516621 172359 0 None 14 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 233 1 1 2 2.8 Cn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
118731354 117687 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 10 0 4 4.9 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(=O)N2CCCCC2)CC1 10.1016/j.ejmech.2014.12.041
CHEMBL3409037 117687 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 496 10 0 4 4.9 CC(C)c1ccccc1N1CCN(CCCCCCC(=O)N2CCC[C@H]2C(=O)N2CCCCC2)CC1 10.1016/j.ejmech.2014.12.041
2600 3720 73 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3720 73 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3720 73 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3720 73 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3720 73 None -5 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
155552826 173520 0 None -37 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 269 3 1 4 2.8 CCn1cncc1-c1c[nH]c2ccc(C(=O)OC)cc12 10.1039/C8MD00313K
CHEMBL4544802 173520 0 None -37 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 269 3 1 4 2.8 CCn1cncc1-c1c[nH]c2ccc(C(=O)OC)cc12 10.1039/C8MD00313K
68108806 131149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 3 2 5 2.3 CNC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692890 131149 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 370 3 2 5 2.3 CNC(=O)c1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
11121216 29925 0 None -30 14 Human 7.2 pKi = 7.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 29925 0 None -30 14 Human 7.2 pKi = 7.2 Binding
Binding affinities towards 5-hydroxytryptamine 6 receptorBinding affinities towards 5-hydroxytryptamine 6 receptor
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
1244725 59178 16 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 417 4 0 6 3.6 CN1CCN(c2oc(-c3ccccc3Cl)nc2S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL1714441 59178 16 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 417 4 0 6 3.6 CN1CCN(c2oc(-c3ccccc3Cl)nc2S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2019.111857
2865 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
59 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
60854 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
CHEMBL708 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
DB00246 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) by radioligand binding assayBinding affinity to 5HT6 receptor (unknown origin) by radioligand binding assay
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm400856t
155555506 173810 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 2 5.1 CN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
CHEMBL4552041 173810 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 330 6 1 2 5.1 CN(CCc1c[nH]c2ccccc12)Cc1ccc(-c2ccccc2)o1 10.1016/j.ejmech.2019.111857
126720410 162361 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1F 10.1016/j.ejmech.2017.12.053
CHEMBL4173960 162361 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1F 10.1016/j.ejmech.2017.12.053
2865 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
59 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
60854 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
CHEMBL708 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
DB00246 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmcl.2010.07.105
2906559 93977 11 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 316 5 1 6 2.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL251005 93977 11 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 316 5 1 6 2.6 CN1CCN(c2ccc([N+](=O)[O-])c(NCc3ccco3)c2)CC1 10.1016/j.bmcl.2007.09.016
145961959 160948 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4128013 160948 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 467 3 1 5 4.6 O=S(=O)(c1cccc(Br)c1)n1cc(C2=CCNCC2)c2ccc3cccnc3c21 10.1016/j.bmc.2018.05.033
5 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
56945045 111569 0 None -7 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 8 1 6 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
CHEMBL3289956 111569 0 None -7 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 514 8 1 6 5.0 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2cc(Cl)ccc2c1 10.1021/jm401895u
71456944 81649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 486 3 0 4 4.5 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2F)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165564 81649 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 486 3 0 4 4.5 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2ccc(F)c(F)c2F)C1 10.1016/j.bmcl.2012.06.002
25263309 183523 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL482568 183523 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 350 4 1 3 4.3 Cc1c(OCc2ccc(Cl)c(Cl)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
162659577 180776 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4763106 180776 0 None -6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
44401390 124111 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 223 2 1 1 3.5 Nc1ccc(CC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL364089 124111 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 223 2 1 1 3.5 Nc1ccc(CC2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
134134456 142812 0 None -23 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 514 11 1 5 5.4 COc1ccc(-c2cc(F)ccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3897426 142812 0 None -23 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 514 11 1 5 5.4 COc1ccc(-c2cc(F)ccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11849196 79779 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1cccc(N2CCNCC2)c1)c1ccccc1 10.1021/jm060469q
CHEMBL213586 79779 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1cccc(N2CCNCC2)c1)c1ccccc1 10.1021/jm060469q
145953693 162048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 375 3 1 5 3.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4169050 162048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 375 3 1 5 3.2 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(C(F)(F)F)c1 10.1016/j.ejmech.2017.12.053
118731513 117747 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 477 11 2 6 3.6 NC(=O)c1ccccc1OCCCNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
CHEMBL3409248 117747 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 477 11 2 6 3.6 NC(=O)c1ccccc1OCCCNCCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
24794436 13955 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL1197511 13955 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
CHEMBL574856 13955 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 393 4 4 4 2.8 N=C(N)N/N=C1\CCc2ccc(NS(=O)(=O)c3ccc4ccccc4c3)cc21 10.1021/jm900796p
10199220 18306 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 266 4 0 4 1.6 CN(C)CCc1cn(S(C)(=O)=O)c2ccccc12 10.1021/jm010943m
CHEMBL127232 18306 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 266 4 0 4 1.6 CN(C)CCc1cn(S(C)(=O)=O)c2ccccc12 10.1021/jm010943m
216239 23591 114 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 23591 114 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 23591 114 None -9 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
5323 201101 99 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
CHEMBL62193 201101 99 None - 1 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 nan
145983390 165366 0 None -204 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1ccnc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4250274 165366 0 None -204 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 535 6 0 7 5.0 O=S(=O)(c1ccnc2ccccc12)N1CCCCC[C@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
155522563 176082 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4453687 176082 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598088 176082 0 None -13 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 483 8 0 4 5.4 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/j.bmc.2019.06.028
71450247 82563 0 None -1258 9 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT6 by Cerep protocol based assayBinding affinity to human 5HT6 by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181188 82563 0 None -1258 9 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT6 by Cerep protocol based assayBinding affinity to human 5HT6 by Cerep protocol based assay
ChEMBL 368 5 0 3 5.5 CCCN1CCC(COc2nc3c(Cl)cccc3c3ccccc23)CC1 10.1021/jm300943r
145977256 162997 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 391 4 1 3 3.5 O=C1Nc2ccccc2C12CCN(CCN1CC=C(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4202947 162997 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 391 4 1 3 3.5 O=C1Nc2ccccc2C12CCN(CCN1CC=C(c3ccc(F)cc3)CC1)C2 10.1016/j.bmcl.2018.06.019
122186880 122465 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 122465 0 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
44389999 13800 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL1196367 13800 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
CHEMBL556760 13800 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 299 3 2 4 3.5 O=S(=O)(c1ccc(NO)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2005.01.031
10269916 16696 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 360 6 0 4 2.9 COc1ccc2c(c1)C(CCN(C)C)CN2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL124971 16696 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 360 6 0 4 2.9 COc1ccc2c(c1)C(CCN(C)C)CN2S(=O)(=O)c1ccccc1 10.1021/jm010943m
72197845 89414 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
CHEMBL2377590 89414 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2019.111736
72197845 89414 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
CHEMBL2377590 89414 0 None -8 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 486 7 2 3 5.3 O=C1CC(c2c[nH]c3ccccc23)C(=O)N1CCCCN1CCC(c2c[nH]c3ccc(F)cc23)CC1 10.1016/j.ejmech.2013.02.033
66801000 111570 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 472 7 1 7 4.0 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3289957 111570 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 472 7 1 7 4.0 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
10500364 201180 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 386 5 1 6 2.1 COc1ccc(NS(=O)(=O)c2cccc(C#N)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL62594 201180 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 386 5 1 6 2.1 COc1ccc(NS(=O)(=O)c2cccc(C#N)c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10637020 67298 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2cccc3[nH]ccc23)cc1 10.1021/jm050247c
CHEMBL190521 67298 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 287 3 3 3 2.6 Nc1ccc(S(=O)(=O)Nc2cccc3[nH]ccc23)cc1 10.1021/jm050247c
44398455 67306 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 5 4.6 Cc1c(S(=O)(=O)Nc2cccc3c2ccn3CCN)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL190594 67306 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 419 5 2 5 4.6 Cc1c(S(=O)(=O)Nc2cccc3c2ccn3CCN)sc2ccc(Cl)cc12 10.1021/jm050247c
162662361 180890 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4764557 180890 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 465 8 1 6 4.0 COc1ccc2cc(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)ccc2c1 10.1016/j.ejmech.2020.112149
2865 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 4079 67 None -83 53 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
23653130 56404 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 463 6 0 7 3.7 CCN1CCN(c2cn(S(=O)(=O)c3cc(OC)ccc3OC)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642429 56404 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 463 6 0 7 3.7 CCN1CCN(c2cn(S(=O)(=O)c3cc(OC)ccc3OC)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
235964 123505 6 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 263 3 3 4 1.7 Nc1ccc(S(=O)(=O)Nc2cccc(N)c2)cc1 10.1021/jm050247c
CHEMBL362984 123505 6 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 263 3 3 4 1.7 Nc1ccc(S(=O)(=O)Nc2cccc(N)c2)cc1 10.1021/jm050247c
23625925 93138 0 None -295 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
CHEMBL246484 93138 0 None -295 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
44441238 93279 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 2 1 4 2.0 Nc1cccc2c1OCCN2S(=O)(=O)c1ccccc1F 10.1016/j.bmcl.2006.12.093
CHEMBL247119 93279 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 308 2 1 4 2.0 Nc1cccc2c1OCCN2S(=O)(=O)c1ccccc1F 10.1016/j.bmcl.2006.12.093
3233 3456 40 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3456 40 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3456 40 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3456 40 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3456 40 None -4677 12 Human 5.2 pKi = 5.2 Binding
Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
142601335 185839 0 None -52 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4876193 185839 0 None -52 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
21514234 167976 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2004.01.071
CHEMBL435534 167976 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 318 4 0 2 4.7 CN(C)CC1CCCc2c1c1ccccc1n2Cc1ccccc1 10.1016/j.bmcl.2004.01.071
68342091 127448 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 6 4.0 COCCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
CHEMBL3664795 127448 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 449 5 1 6 4.0 COCCn1ccc2cc(S(=O)(=O)c3ccc4c(c3)c3c(n4C)CC4CCC3N4)ccc21 nan
137637698 155279 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4059916 155279 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3cccc(F)c3)n2)CC1 10.1016/j.ejmech.2017.04.033
137651330 156936 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
CHEMBL4079397 156936 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccc(Cc2nc(N)nc(N3CCN(C)CC3)n2)cc1 10.1016/j.ejmech.2017.04.033
137659459 158585 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 5 3.2 Cc1ccc(C)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4097882 158585 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 397 4 0 5 3.2 Cc1ccc(C)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
137662033 158605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(F)cccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4098120 158605 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 405 4 0 5 2.9 CN1CCN(Cc2cn(S(=O)(=O)c3c(F)cccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
22662986 84870 48 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 161 2 2 2 1.1 NCCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260372 84870 48 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 161 2 2 2 1.1 NCCc1c[nH]c2ccncc12 10.1007/s00044-004-0121-8
44263497 198321 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 4 1 6 4.2 COc1cc2c(cc1NS(=O)(=O)c1c(Cl)nc3sccn13)C(C)=C(C)C2 10.1016/j.bmc.2009.08.006
CHEMBL595301 198321 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 409 4 1 6 4.2 COc1cc2c(cc1NS(=O)(=O)c1c(Cl)nc3sccn13)C(C)=C(C)C2 10.1016/j.bmc.2009.08.006
24784321 190415 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1ccc(F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL518670 190415 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 361 3 1 6 2.2 O=S(=O)(c1ccc(F)cc1)c1cccc2oc(N3CCNCC3)nc12 10.1016/j.bmcl.2008.12.107
57403837 71129 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1949772 71129 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
CHEMBL1962399 71129 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 329 2 1 4 2.7 Cc1ccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)cc1 10.1016/j.bmcl.2011.12.026
68115859 131745 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2ccnc2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3696980 131745 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 393 4 1 6 3.2 O=S(=O)(c1ccccc1)c1cc(Cn2ccnc2)c2oc3c(c2c1)CNCC3 nan
11269402 60213 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3cccc4ccccc34)cccc21 10.1021/jm049615n
CHEMBL175819 60213 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2c(NS(=O)(=O)c3cccc4ccccc34)cccc21 10.1021/jm049615n
44397420 12895 25 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL1189727 12895 25 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL539327 12895 25 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
6476992 69135 8 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 219 1 1 1 3.8 Nc1ccc(/C=C2\C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL193376 69135 8 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 219 1 1 1 3.8 Nc1ccc(/C=C2\C=Cc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
134157171 153404 0 None -99 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 1 6 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccc(OC)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3983496 153404 0 None -99 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 531 14 1 6 5.3 COCOc1ccc(CNC(=O)CCCCCN2CCN(c3ccccc3-c3ccc(OC)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
137645501 157103 0 None -16 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4081383 157103 0 None -16 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 4.9 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
2870750 117427 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 442 4 1 5 6.0 Nc1c(S(=O)(=O)c2ccccc2)sc2nc(-c3ccccc3)cc(-c3ccccc3)c12 10.1016/j.bmcl.2015.03.049
CHEMBL3403334 117427 7 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 442 4 1 5 6.0 Nc1c(S(=O)(=O)c2ccccc2)sc2nc(-c3ccccc3)cc(-c3ccccc3)c12 10.1016/j.bmcl.2015.03.049
145983128 165272 0 None -128 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248597 165272 0 None -128 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
127037681 136091 0 None -33 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 406 8 1 6 2.4 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cnn(C)c2)CC1 10.1039/C5MD00166H
CHEMBL3739745 136091 0 None -33 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assayDisplacement of [3H]-LSD from human serotonin 5-HT6 receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
ChEMBL 406 8 1 6 2.4 CC(C)c1ccccc1OCCN1CCC(NS(=O)(=O)c2cnn(C)c2)CC1 10.1039/C5MD00166H
68108546 131162 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 295 3 1 4 3.9 COc1cc(Oc2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692903 131162 0 None - 1 Human 6.2 pKi = 6.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 295 3 1 4 3.9 COc1cc(Oc2ccccc2)cc2c3c(oc12)CCNC3 nan
139488518 169430 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cccc(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4442337 169430 0 None -16 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 229 2 1 2 3.2 CCn1cncc1-c1c[nH]c2cccc(F)c12 10.1016/j.ejmech.2019.03.017
44278114 99742 0 None -954 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28833 99742 0 None -954 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
164612518 184812 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4860719 184812 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3cccc(Cl)c3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
5 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
180 397 50 None -99 38 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -99 38 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -99 38 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -99 38 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -99 38 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
53326048 59815 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1642869 59815 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
CHEMBL1739584 59815 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 450 8 2 5 4.2 CCN(CC)CCC(=O)Nc1ccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c2c1 10.1016/j.bmc.2010.10.033
162648765 179180 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
CHEMBL4744372 179180 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2020.112916
162654919 179982 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 603 14 2 8 4.2 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4754024 179982 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 603 14 2 8 4.2 C[C@H](NCc1ccc(OCCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
155534040 171364 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4470226 171364 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 449 4 1 7 5.1 COc1ccc2c(c1)c(-c1nc(N)sc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
57391669 71218 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949677 71218 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1963079 71218 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 391 4 1 5 3.3 CC(C)Oc1cc(F)cc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
90656155 110337 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 2 4.0 Clc1ccccc1C1CCN(c2ccc3c(c2)CCNCC3)C1 10.1016/j.bmcl.2014.03.049
CHEMBL3260787 110337 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 326 2 1 2 4.0 Clc1ccccc1C1CCN(c2ccc3c(c2)CCNCC3)C1 10.1016/j.bmcl.2014.03.049
22425072 117437 6 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 457 5 0 4 6.5 Cc1ccc(S(=O)(=O)c2cnc3ccc(F)cc3c2SCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403343 117437 6 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 457 5 0 4 6.5 Cc1ccc(S(=O)(=O)c2cnc3ccc(F)cc3c2SCc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2015.03.049
4211 57517 81 None 1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
CHEMBL1670 57517 81 None 1 4 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 nan
134137560 142173 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3892201 142173 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
117209962 184286 1 None -25 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184286 1 None -25 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
57391158 71213 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1949979 71213 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
CHEMBL1963033 71213 0 None -10 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 444 7 1 5 3.4 O=S(=O)(NCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cnc2ccccc2c1 10.1016/j.bmc.2011.12.039
145975905 163276 0 None -66 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
CHEMBL4206366 163276 0 None -66 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 376 4 1 4 2.4 O=C1Nc2ccccc2C12CCN(CCN1CCN(c3ccccc3)CC1)C2 10.1016/j.bmcl.2018.06.019
16118929 59840 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1642860 59840 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
CHEMBL1739698 59840 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 406 4 3 5 3.7 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2c(NC3CCCNC3)cccc12 10.1016/j.bmc.2010.10.033
24763353 62296 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783603 62296 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2009.04.108
66801271 111613 0 None -74 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
CHEMBL3289999 111613 0 None -74 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 423 7 1 6 3.6 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccs1 10.1021/jm401895u
68115698 131212 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3692953 131212 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 432 4 0 5 3.4 CN(C)CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
45488139 195272 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
CHEMBL566410 195272 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 306 3 1 3 2.9 CN1CCN(c2cccc3[nH]c(Cc4ccccc4)nc23)CC1 10.1021/jm901672k
168282733 190465 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 386 9 3 9 1.4 COc1ccccc1N1CCN(CCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5187317 190465 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 386 9 3 9 1.4 COc1ccccc1N1CCN(CCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
66801528 156301 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
CHEMBL4071451 156301 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 449 6 2 3 4.5 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1)c1ccc2ccccc2c1 10.1021/acs.jmedchem.7b00839
155569568 175620 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 380 7 2 3 5.4 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(Cl)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
CHEMBL4593671 175620 0 None 3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 380 7 2 3 5.4 COc1ccc2[nH]cc(CCNCc3ccc(-c4ccc(Cl)cc4)o3)c2c1 10.1016/j.ejmech.2019.111857
118654425 189983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
CHEMBL5180275 189983 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis
ChEMBL 421 5 1 6 3.2 COc1ccc(S(=O)(=O)n2cc(C(F)F)c3cc(N4CCNCC4)ccc32)cc1 10.1016/j.bmc.2022.116950
2948971 72864 9 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL2011865 72864 9 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrationsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells using seven compounds concentrations
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
155562202 175245 0 None -67 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4584719 175245 0 None -67 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 471 9 0 5 4.8 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2019.06.029
137649997 156747 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4076903 156747 0 None -32 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 464 6 0 5 3.8 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccccc3)CC2)CC1 10.1016/j.bmc.2017.04.046
44567985 191797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL520777 191797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 340 2 1 4 2.9 Cc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCNCC3)c1 10.1016/j.bmcl.2008.06.030
162656667 180276 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 589 13 2 8 3.8 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
CHEMBL4757296 180276 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 589 13 2 8 3.8 C[C@H](NCc1ccc(OCCCCN2CCN(c3cccc4c3ccn4S(=O)(=O)c3ccccc3)CC2)cc1)C(N)=O 10.1016/j.ejmech.2020.112765
46880530 6221 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 402 4 0 5 3.9 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCN(C)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081792 6221 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 402 4 0 5 3.9 COc1ccc2c(c1)c(S(=O)(=O)c1cccc(F)c1)cn2C1CCCN(C)C1 10.1016/j.bmcl.2010.01.073
118724637 120102 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3360997 120102 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546115 120102 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 464 6 0 8 2.3 Cn1c(=O)c2c(ncn2CCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n(C)c1=O 10.1016/j.bmc.2014.11.008
57391567 71193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949927 71193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962944 71193 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 367 2 1 4 3.2 O=S(=O)(c1cc(F)cc(Cl)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
52915868 60660 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
CHEMBL1762570 60660 6 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptorDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 10.1016/j.ejmech.2011.01.038
52915868 60660 6 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
CHEMBL1762570 60660 6 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.Radioligand Binding Assay: Radioligand binding assay using 5-HT6 receptors.
ChEMBL 301 2 0 5 2.5 Cc1cc(C)n2nc(C)c(S(=O)(=O)c3ccccc3)c2n1 nan
168293874 191581 0 None -15 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 191581 0 None -15 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
118731512 117746 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 427 11 2 4 4.4 NC(=O)c1ccccc1OCCCNCCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
CHEMBL3409247 117746 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 427 11 2 4 4.4 NC(=O)c1ccccc1OCCCNCCc1cn(Cc2ccccc2)c2ccccc12 10.1016/j.ejmech.2014.12.045
66801229 111565 0 None -758 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
CHEMBL3289952 111565 0 None -758 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 452 6 1 6 3.6 O=S(=O)(NCCN1CCN(c2nsc3ccccc23)CC1)c1ccc2ccccc2c1 10.1021/jm401895u
155554325 175947 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4548353 175947 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4597000 175947 0 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 447 8 0 3 5.8 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2019.06.028
155552641 173569 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 3 1 6 5.0 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4546365 173569 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 419 3 1 6 5.0 Cc1sc(N)nc1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
127036932 136824 0 None -2 22 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 136824 0 None -2 22 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
155562652 174589 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 552 9 1 7 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccc(OC)cc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
CHEMBL4570209 174589 0 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 552 9 1 7 5.3 COc1ccc(-c2c(=O)n(CCCCN3CCCC(c4c[nH]c5ccc(OC)cc45)C3)c(=O)n3ccccc23)cc1 10.1016/j.ejmech.2019.01.031
130442572 171342 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
155537034 171719 0 None -1148 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 240 2 2 3 1.7 Cn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1039/C8MD00313K
CHEMBL4474827 171719 0 None -1148 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 240 2 2 3 1.7 Cn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1039/C8MD00313K
138691338 163115 0 None -229 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 241 3 1 3 3.1 CCn1cncc1-c1c[nH]c2ccc(OC)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4204595 163115 0 None -229 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 241 3 1 3 3.1 CCn1cncc1-c1c[nH]c2ccc(OC)cc12 10.1016/j.ejmech.2019.03.017
155522511 170160 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1OC 10.1016/j.ejmech.2019.111857
CHEMBL4452149 170160 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1OC 10.1016/j.ejmech.2019.111857
164615243 184627 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4857676 184627 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
168288135 191152 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.5 Clc1cccc(Cn2ccc3c(NCC4CCCO4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5197407 191152 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.5 Clc1cccc(Cn2ccc3c(NCC4CCCO4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
752521 197060 7 None -33 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 197060 7 None -33 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT6 receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
155528967 170826 0 None -15 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 510 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
CHEMBL4462139 170826 0 None -15 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 510 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2ccccn2c(=O)n1CCCCN1CCCC(c2c[nH]c3ccccc23)C1 10.1016/j.ejmech.2019.01.031
44388944 62689 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
CHEMBL178767 62689 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 431 3 2 5 3.6 Nc1ccc(S(=O)(=O)n2cc(C3=CCNCC3)c3cc(Br)ccc32)cc1 10.1016/j.bmcl.2004.10.064
155540062 172340 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 339 4 2 7 1.3 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)N(C)NC3)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4516220 172340 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 339 4 2 7 1.3 CN1CCN(c2nc(NCc3ccccc3)c3c(n2)N(C)NC3)CC1 10.1016/j.ejmech.2019.111857
67003550 192099 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constant
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1CN1CCN(C)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219467 192099 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H] LSD from recombinant human 5-HT6R expressed in HEK293 cells assessed as inhibition constant
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3ccccc32)cc1CN1CCN(C)CC1 10.1016/j.bmcl.2021.128275
155557760 174079 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4558433 174079 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2ccccc21 10.1021/acsmedchemlett.6b00056
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2018.01.002
155531065 171047 0 None 24 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 3 3 4.5 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4465414 171047 0 None 24 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 332 6 3 3 4.5 Oc1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.022
90469185 184979 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 4 1 7 2.8 COc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
CHEMBL4863272 184979 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 422 4 1 7 2.8 COc1cccc(S(=O)(=O)n2ccc3c(N4CCNCC4)nc4ccccc4c32)c1 10.1021/acs.jmedchem.1c00224
90109808 181783 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 325 3 1 3 3.8 Clc1cccc(Cn2ccc3c(N4CCNCC4)cccc32)c1 10.1016/j.ejmech.2020.112765
CHEMBL4784859 181783 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 325 3 1 3 3.8 Clc1cccc(Cn2ccc3c(N4CCNCC4)cccc32)c1 10.1016/j.ejmech.2020.112765
164616626 183969 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 582 13 2 7 6.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4848231 183969 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 582 13 2 7 6.6 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
126720394 161764 0 None 63 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4164541 161764 0 None 63 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 355 4 1 5 3.1 CCc1nc2c(N3CCNCC3)ccnc2n1Cc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2014.01.065
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysisDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.01.031
44403093 71094 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL196094 71094 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 388 4 0 4 4.2 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10177537 123857 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363843 123857 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 376 3 1 4 3.6 O=S(=O)(c1ccc(F)c(F)c1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44403089 133106 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL371469 133106 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 432 4 0 4 4.3 CN1CCC[C@H]1Cc1cn(S(=O)(=O)c2ccccc2Br)c2ccccc12 10.1016/j.bmcl.2005.07.028
44403065 165759 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL427184 165759 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 355 4 2 5 2.8 Nc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.07.027
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2020.112529
164615124 184419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2021.113792
CHEMBL4854568 184419 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 513 8 1 7 4.5 CC(C)(C)OC(=O)N1CCC(CNCCOc2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2021.113792
44405348 140773 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
CHEMBL383354 140773 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 301 3 2 5 2.5 CNc1ccc2ccn(S(=O)(=O)c3ccc(N)cc3)c2c1 10.1016/j.bmcl.2005.08.059
23655467 88960 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
CHEMBL236988 88960 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 360 6 1 6 2.4 COc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1OC 10.1021/jm070521y
23655469 88962 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
CHEMBL236990 88962 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 384 4 1 5 3.2 NCCc1cn(S(=O)(=O)c2ccc(Br)s2)c2ccccc12 10.1021/jm070521y
127046817 139069 0 None 28 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 437 5 0 7 3.2 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C#N)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3797435 139069 0 None 28 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 437 5 0 7 3.2 CC(C)CS(=O)(=O)n1ccc2c(-c3ccc(C#N)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
127047537 139377 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 508 4 0 7 3.8 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCOCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
CHEMBL3799448 139377 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 508 4 0 7 3.8 CN1CCN(c2cc(-c3ccc(C(F)(F)F)cc3)c3ccn(S(=O)(=O)C4CCOCC4)c3n2)CC1 10.1016/j.bmcl.2016.04.024
135398745 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
47 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
CHEMBL715 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
DB00334 2869 108 None -4 65 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2014.11.008
11441983 200104 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606818 200104 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 437 5 2 3 4.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc12 10.1021/jm049243i
73453 29403 22 None -10 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29403 22 None -10 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
58258793 127412 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 2 1 4 4.0 Cc1cccc(S(=O)(=O)c2cc(C)c3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
CHEMBL3664758 127412 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 380 2 1 4 4.0 Cc1cccc(S(=O)(=O)c2cc(C)c3c(c2)c2c(n3C)CC3CCC2N3)c1 nan
58258791 128469 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128469 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
44240753 138580 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786693 138580 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 363 3 2 4 2.2 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC2(C=N1)CCCCC2 10.1016/j.bmcl.2016.02.001
46880606 5896 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1079976 5896 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 404 3 0 4 4.9 CN1CCCC(n2cc(S(=O)(=O)c3cccc4ccccc34)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
24783294 176138 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
CHEMBL459987 176138 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 393 3 1 6 3.2 O=S(=O)(c1cccc2ccccc12)c1cccc2nc(N3CCNCC3)oc12 10.1016/j.bmcl.2008.12.107
66801346 111607 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289993 111607 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 485 7 1 5 4.8 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
6918601 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm5003952
CHEMBL127411 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm5003952
58258835 128443 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc2ccccc2n1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
CHEMBL3669642 128443 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 405 2 1 5 4.0 Cc1cc2ccccc2n1S(=O)(=O)c1ccc2c(c1)c1c(n2C)CC2CCC1N2 nan
6918601 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
CHEMBL127411 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
6918601 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL127411 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1016/j.bmcl.2012.06.002
44327527 108006 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 2 2 5 2.1 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N)C3)cc1 10.1021/jm030030n
CHEMBL319956 108006 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 2 2 5 2.1 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N)C3)cc1 10.1021/jm030030n
59339335 138477 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3785626 138477 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 323 4 2 4 1.3 CCN/C(=N\S(=O)(=O)c1ccc(N)cc1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56593934 65364 0 None 2630 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
CHEMBL1834350 65364 0 None 2630 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 383 3 2 4 1.7 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCNCC2 10.1021/jm200466r
52913218 70418 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950763 70418 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4cccc(OC(F)(F)F)c4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
11317551 60167 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 477 12 2 3 6.6 CCCCN(CCCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
CHEMBL175529 60167 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 477 12 2 3 6.6 CCCCN(CCCC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cccc4ccccc34)cc12 10.1021/jm049615n
9999118 6092 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
CHEMBL1081094 6092 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 368 4 0 4 4.1 CCN1CCCC(n2cc(S(=O)(=O)c3ccccc3)c3ccccc32)C1 10.1016/j.bmcl.2010.01.073
71151953 117741 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 542 9 1 5 6.2 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
CHEMBL3409242 117741 0 None -5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 542 9 1 5 6.2 O=C1CCc2ccc(OCCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cc2N1 10.1016/j.ejmech.2014.12.045
12017572 203165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3c(OC)cccc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL75758 203165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3c(OC)cccc32)c1 10.1016/s0960-894x(00)00453-4
68115749 131747 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696982 131747 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 327 3 1 4 3.3 COc1cc([S+]([O-])c2ccccc2)cc2c3c(oc12)CCNC3 nan
58258756 127435 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664782 127435 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 408 2 1 5 4.6 Cn1c2c(c3cc(S(=O)(=O)c4ccc5sccc5c4)ccc31)C1CCC(C2)N1 nan
66852770 158324 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4095054 158324 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1cc(CN2CCNCC2)c2ccccc21 10.1021/acs.jmedchem.6b01662
16222651 81643 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 474 4 0 4 5.2 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165558 81643 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 474 4 0 4 5.2 CC(C)c1ccc(S(=O)(=O)n2c3c(c4cc(Br)ccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
44537940 18587 0 None 18 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
CHEMBL1278001 18587 0 None 18 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 482 5 1 6 4.5 O=S(=O)(c1cccc2ccccc12)c1nn(Cc2ccccc2)c2ccc(N3CCNCC3)cc12 10.1021/jm1007825
68108970 131165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 2 1 2 4.9 CC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692906 131165 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 311 2 1 2 4.9 CC(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
134551 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
44435630 89246 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL237593 89246 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
162651486 179689 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4750587 179689 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 437 7 1 5 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc(F)c(Cl)c1 10.1016/j.ejmech.2020.112149
44386822 165433 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 449 5 0 6 4.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3cccnc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL425328 165433 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 449 5 0 6 4.4 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2cccc3cccnc23)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44435630 89246 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL237593 89246 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 375 3 1 5 3.4 O=S(=O)(c1ccc(Cl)cc1)c1cn(C2CCCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
71502631 117759 0 None 38 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 475 8 0 6 4.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
CHEMBL3409260 117759 0 None 38 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 475 8 0 6 4.5 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCOc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2014.12.045
57414666 131199 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1ccc(C(O)C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692940 131199 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 445 3 2 5 4.2 O=S(=O)(c1ccc(C(O)C(F)(F)F)cc1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
68115687 131223 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692964 131223 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 1 5 3.6 O=S(=O)(c1ccc2c(c1)COC2)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
58149663 126900 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
CHEMBL3659969 126900 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.Competitive Binding Assay: Activity test of serotonin 5-HT6 receptor antagonists of the general formulas 1, 2 in the setting of competitive binding to serotonin 5-HT6 receptors.
ChEMBL 374 3 1 7 2.2 CSc1nn2c3c(c(C)nc2c1S(=O)(=O)c1ccccc1)CNCC3 nan
57391729 69403 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
CHEMBL1935593 69403 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from full length human 5HT6 receptorDisplacement of [3H]LSD from full length human 5HT6 receptor
ChEMBL 341 2 1 4 3.6 CC1(C)NCCc2c1oc1cc(S(=O)(=O)c3ccccc3)ccc21 10.1016/j.bmcl.2011.11.050
58149665 81932 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
CHEMBL2172183 81932 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 minsDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor expressed in HeLa cells after 120 mins
ChEMBL 374 3 0 7 2.3 CSc1nn2c3c(cnc2c1S(=O)(=O)c1ccccc1)CN(C)CC3 10.1016/j.bmcl.2012.05.036
68115874 131735 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 5 2 6 2.7 CC(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696970 131735 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 5 2 6 2.7 CC(O)COc1cc(S(=O)(=O)c2ccccc2)cc2c3c(oc12)CCNC3 nan
CHEMBL5088232 213372 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2ccc3ccccc3c2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
25024926 62634 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
CHEMBL1785067 62634 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 4 1 5 3.0 O=S(=O)(c1ccccc1Br)n1ccc2cc(CN3CCNCC3)ccc21 10.1021/ml100101u
137630441 160517 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4083893 160517 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4116632 160517 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 5 0 6 3.2 COc1ccc2c(c1)c(CN1CCCN(C)CC1)cn2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01662
52912973 70405 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
CHEMBL1950750 70405 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 nan
57394331 70406 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 nan
CHEMBL1950751 70406 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 nan
44397392 11670 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1181693 11670 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL188864 11670 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 340 4 1 4 3.2 O=S(=O)(c1ccccc1)n1cc(C[C@H]2CCCN2)c2ccccc21 10.1016/j.bmcl.2005.05.092
137653219 158112 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 449 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/acs.jmedchem.6b01662
CHEMBL4092681 158112 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 449 5 0 6 3.8 COc1ccc2c(c1)c(CN1CCN(C)CC1)cn2S(=O)(=O)c1cccc2ccccc12 10.1021/acs.jmedchem.6b01662
137656608 159062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4103281 159062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccccc3F)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
57394331 70406 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
CHEMBL1950751 70406 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 366 2 0 4 3.7 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
49836715 18475 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
CHEMBL1277010 18475 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 362 3 1 6 2.2 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccs4)c3c2)CC1 10.1021/jm1007825
53322548 56393 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642418 56393 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 467 3 0 5 4.0 CN1CCN(c2cn(S(=O)(=O)c3cccc(Cl)c3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
24775945 84103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL2220318 84103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
CHEMBL3216565 84103 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 355 4 1 5 2.3 O=S(=O)(c1ccccc1)n1ccc2c(CN3CCNCC3)cccc21 10.1016/j.bmcl.2012.10.057
9906059 206449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cellsBinding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL98404 206449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cellsBinding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
9908552 18400 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc(Cl)c1 10.1021/jm010943m
CHEMBL127636 18400 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 392 6 0 5 3.6 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccc(Cl)c1 10.1021/jm010943m
9906059 206449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
CHEMBL98404 206449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 342 6 0 4 3.4 CN(C)CCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm030030n
56595402 65306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL1834226 65306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
56595402 65306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834226 65306 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 342 4 1 3 2.3 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56595671 65347 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834333 65347 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 376 4 1 3 3.0 CCN/C(=N\S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CC(CC)C=N1 10.1021/jm200466r
56593797 65356 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834341 65356 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 388 4 1 6 2.0 CCN/C(=N\S(=O)(=O)c1c(Cl)nc2sccn12)N1CC(CC)C=N1 10.1021/jm200466r
25263297 183755 0 None 19 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
CHEMBL484345 183755 0 None 19 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 394 5 2 6 2.7 NCCC(=O)Nc1cccc2c1cnn2S(=O)(=O)c1cccc2ccccc12 10.1016/j.bmcl.2009.03.071
24776044 83624 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207389 83624 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
17940234 119494 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccc(C)cc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL350026 119494 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 439 5 2 5 3.0 COc1ccc(S(=O)(=O)Nc2ccc(C)cc2Br)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
9827562 130918 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2cc(Cl)cc(Cl)c2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL369071 130918 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 506 4 2 6 5.3 Cc1sc2cc(Cl)cc(Cl)c2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
6918601 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm050247c
CHEMBL127411 18337 0 None 407 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm050247c
134137152 142533 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@H]1CCO 10.1016/j.bmc.2016.10.010
CHEMBL3895173 142533 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 356 5 2 5 2.6 CN[C@H]1c2c(ccc3c2ccn3S(=O)(=O)c2ccccc2)[C@H]1CCO 10.1016/j.bmc.2016.10.010
46889919 7122 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 3 1 4 2.2 Cn1ccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
CHEMBL1085618 7122 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD form human recombinant 5HT6 receptorDisplacement of [3H]LSD form human recombinant 5HT6 receptor
ChEMBL 304 3 1 4 2.2 Cn1ccc(S(=O)(=O)c2ccc3c(c2)CCC[C@H]3CN)c1 10.1016/j.bmcl.2010.03.110
17978406 71097 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
CHEMBL196103 71097 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 425 3 1 5 4.1 O=S(=O)(c1cccc2ccccc12)n1ccc2c(N3CCNCC3)c(Cl)ccc21 10.1016/j.bmcl.2005.06.107
44403277 165666 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)ccnc12 10.1016/j.bmcl.2005.06.107
CHEMBL426640 165666 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 342 3 2 5 1.8 O=S(=O)(c1ccccc1)c1c[nH]c2c(N3CCNCC3)ccnc12 10.1016/j.bmcl.2005.06.107
135398737 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
135398745 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
17961003 93237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 3 1 5 3.1 CC(C)(C)c1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
CHEMBL246916 93237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
ChEMBL 433 3 1 5 3.1 CC(C)(C)c1cc(N2CCNCC2)c2c(c1)N(S(=O)(=O)c1ccccc1F)CCO2 10.1016/j.bmcl.2006.12.093
44425719 85923 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 483 6 2 4 5.7 CC(C)Nc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
CHEMBL231350 85923 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 483 6 2 4 5.7 CC(C)Nc1cc2c(cc1NS(=O)(=O)c1ccc(-c3ccc(Cl)cc3)cc1)CCN(C)CC2 10.1016/j.bmcl.2006.10.036
44425702 86012 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 444 4 1 3 5.0 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(F)c(Cl)c4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
CHEMBL231431 86012 0 None -1 5 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human recombinant 5HT6 receptorDisplacement of radioligand from human recombinant 5HT6 receptor
ChEMBL 444 4 1 3 5.0 CN1CCc2ccc(NS(=O)(=O)c3ccc(-c4ccc(F)c(Cl)c4)cc3)cc2CC1 10.1016/j.bmcl.2006.10.036
16222965 81613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)cc(F)c3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165529 81613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 390 3 0 4 3.6 CN(C)C1CCc2c(c3cc(F)cc(F)c3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
46884709 7997 3 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
CHEMBL1091208 7997 3 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].Competitive Binding Assay: Determination of tested compounds binding with 5-HT6 receptors was carried out according to the method described in [Monsma F J Jr, Shen Y, Ward R P, Hamblin M W and Sibley D R, Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol. Pharmacol. 43:320-327, 1993].
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 nan
46884709 7997 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
CHEMBL1091208 7997 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 minsDisplacement of [3H]LSD from 5HT6 receptor in humanHeLa cells after 120 mins
ChEMBL 359 3 0 6 3.2 CSc1nn2cc3c(nc2c1S(=O)(=O)c1ccccc1)CCCC3 10.1016/j.bmcl.2010.02.046
58258773 128467 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OC(F)(F)F)c31)C1CCC(C2)N1 nan
CHEMBL3669666 128467 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 436 3 1 5 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OC(F)(F)F)c31)C1CCC(C2)N1 nan
5 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
5202 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
CHEMBL39 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
DB08839 139 66 None -169 54 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1007/s00044-004-0121-8
145 140 48 None -7 29 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
1832 140 48 None -7 29 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
CHEMBL7257 140 48 None -7 29 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
DB14010 140 48 None -7 29 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1007/s00044-004-0121-8
1150 3817 116 None -7 24 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
125 3817 116 None -7 24 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
CHEMBL6640 3817 116 None -7 24 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
DB08653 3817 116 None -7 24 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5-HT6 receptorBinding affinity to Homo sapiens (human) 5-HT6 receptor
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1007/s00044-004-0121-8
11849794 161335 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/jm060469q
CHEMBL415046 161335 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/jm060469q
164608791 183797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 515 8 1 6 4.1 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
CHEMBL4845699 183797 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 515 8 1 6 4.1 CC(C)(C)OC(=O)N1CCCC(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)C1 10.1016/j.ejmech.2021.113792
164618761 185026 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 9 1 6 3.5 CC(=O)Oc1ccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
CHEMBL4863967 185026 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 466 9 1 6 3.5 CC(=O)Oc1ccc(CNCCOc2cccc3c2CCN3S(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2021.113792
11849794 161335 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/acs.jmedchem.7b00085
CHEMBL415046 161335 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 276 5 2 3 2.0 NCCc1cccc(S(=O)(=O)Nc2ccccc2)c1 10.1021/acs.jmedchem.7b00085
90656158 110340 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 320 3 1 2 3.7 O=C1CC(c2ccccc2)CN1c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260790 110340 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 320 3 1 2 3.7 O=C1CC(c2ccccc2)CN1c1cccc(C2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
45483628 196734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 440 4 3 8 1.5 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N\NC3=NCCN3)CC4)cc21 10.1021/jm900796p
CHEMBL576967 196734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation countingDisplacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
ChEMBL 440 4 3 8 1.5 CN1CCOc2ccc(S(=O)(=O)Nc3ccc4c(c3)/C(=N\NC3=NCCN3)CC4)cc21 10.1021/jm900796p
56944473 111636 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 488 8 1 7 4.5 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
CHEMBL3290021 111636 0 None -8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 488 8 1 7 4.5 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2scnc12 10.1021/jm401895u
71456943 81648 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 534 3 0 4 5.7 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165563 81648 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 534 3 0 4 5.7 CN(C)C1CCc2c(c3cc(Br)ccc3n2S(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)C1 10.1016/j.bmcl.2012.06.002
25263312 184068 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL484965 184068 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 296 4 1 3 3.5 Cc1c(O[C@H](C)c2ccccc2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
134156305 153715 0 None -36 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3986254 153715 0 None -36 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
164623281 185230 0 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 447 7 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4867109 185230 0 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 447 7 0 5 3.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
2585 790 100 None -109 22 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 790 100 None -109 22 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 790 100 None -109 22 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 790 100 None -109 22 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 790 100 None -109 22 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
1548953 205945 24 None -3 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
CHEMBL954 205945 24 None -3 17 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(/C(=C(/Cl)c2ccccc2)c2ccccc2)cc1 nan
155545625 172889 0 None -102 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 255 4 1 3 3.5 CCOc1ccc2[nH]cc(-c3cncn3CC)c2c1 10.1016/j.ejmech.2019.03.017
CHEMBL4529615 172889 0 None -102 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 255 4 1 3 3.5 CCOc1ccc2[nH]cc(-c3cncn3CC)c2c1 10.1016/j.ejmech.2019.03.017
164619936 185627 0 None -1174 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 415 7 0 7 1.6 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4873100 185627 0 None -1174 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 415 7 0 7 1.6 O=C1c2ccccc2S(=O)(=O)N1CCCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2021.128028
16362 3076 67 None -173 29 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
2172 3076 67 None -173 29 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
90 3076 67 None -173 29 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
CHEMBL1423 3076 67 None -173 29 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
DB01100 3076 67 None -173 29 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm030030n
155524228 170308 0 None -21 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(F)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4454176 170308 0 None -21 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CCN(CCCCN4C(=O)CC(c5c[nH]c6ccc(F)cc56)C4=O)CC3)c2c1 10.1016/j.ejmech.2019.111736
155548205 173178 0 None -2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4536834 173178 0 None -2 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 384 5 0 3 4.0 CCCN1CCC(c2ccc3c(c2)N(S(=O)(=O)c2ccccc2)CC3)CC1 10.1016/j.bmcl.2016.07.055
56943891 111559 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
CHEMBL3289946 111559 0 None -10 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 498 8 1 6 4.5 O=S(=O)(NCCCCN1CCN(c2nsc3ccccc23)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm401895u
56593933 65363 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
CHEMBL1834349 65363 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 384 3 1 4 2.1 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC2(C=N1)CCOCC2 10.1021/jm200466r
155546190 175911 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4530770 175911 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4596654 175911 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 467 8 0 4 4.9 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2F)CC1 10.1016/j.bmc.2019.06.028
19958494 98994 0 None -208 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL283036 98994 0 None -208 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
145963649 160975 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
CHEMBL4128338 160975 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 389 3 1 5 3.8 O=S(=O)(c1ccccc1)n1cc(C2=CCNCC2)c2ccc3ncccc3c21 10.1016/j.bmc.2018.05.033
117209911 185747 1 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
CHEMBL4874854 185747 1 None -8 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1ccccc1-c1n[nH]cc1N1CCNCC1 10.1021/acs.jmedchem.1c01093
162656041 180142 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4755749 180142 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2020.112916
11508173 94122 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 2 1 3 3.5 CN(C)c1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL251861 94122 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 328 2 1 3 3.5 CN(C)c1cc(Cl)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
118626045 165116 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4244691 165116 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
155514217 169265 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 461 8 0 5 3.9 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4439795 169265 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 461 8 0 5 3.9 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
155551685 174560 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 495 8 0 5 4.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4569757 174560 0 None -4 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 495 8 0 5 4.5 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2021.128028
46880706 6008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(Cl)ccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080694 6008 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 378 3 1 4 3.8 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2cc(Cl)ccc12 10.1016/j.bmcl.2010.01.073
24784824 176215 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 4 0 6 4.5 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460625 176215 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 447 4 0 6 4.5 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
1809 134 28 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 134 28 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 134 28 None -6918 36 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
2948971 72864 9 None 3 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
CHEMBL2011865 72864 9 None 3 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 397 2 3 1 5.6 O=C1Nc2ccc(Cl)cc2C1(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 10.1016/j.bmcl.2015.03.049
146025727 171119 0 None -269 27 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None -269 27 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
134137732 147236 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3932551 147236 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 485 11 1 4 5.9 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccccc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
155541072 172395 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 290 3 2 4 1.7 CCn1cncc1-c1c[nH]c2ccc(S(N)(=O)=O)cc12 10.1039/C8MD00313K
CHEMBL4517552 172395 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 290 3 2 4 1.7 CCn1cncc1-c1c[nH]c2ccc(S(N)(=O)=O)cc12 10.1039/C8MD00313K
155561995 175149 0 None -23 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
CHEMBL4582567 175149 0 None -23 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method
ChEMBL 532 7 1 5 5.4 O=c1c(-c2ccc(F)cc2)c2n(c(=O)n1CCCCN1CCCC(c3c[nH]c4ccc(F)cc34)C1)CCCC2 10.1016/j.ejmech.2019.07.027
11515129 155066 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 3 1 4 2.8 COc1cc2c(c(OC)c1)C(=O)C(C)(c1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.11.045
CHEMBL404552 155066 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 311 3 1 4 2.8 COc1cc2c(c(OC)c1)C(=O)C(C)(c1ccccc1)C(=O)N2 10.1016/j.bmcl.2007.11.045
10251906 67441 14 None -588 7 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL1908863 67441 14 None -588 7 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
CHEMBL482496 67441 14 None -588 7 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 427 8 1 4 3.6 COc1cc(CCNCc2ccccc2OC)c(OC)cc1I 10.1016/j.bmc.2008.04.050
168283351 190202 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 427 4 1 6 4.3 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCOC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
CHEMBL5183690 190202 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 427 4 1 6 4.3 O=S(=O)(c1cccc(Cl)c1)n1ccc2c(N[C@H]3CCOC3)nc3ccccc3c21 10.1016/j.ejmech.2022.114329
164624803 185630 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4873127 185630 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cccc(Cl)c1Cl)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
11703226 94121 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 2 1 3 3.6 COc1cc(Br)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
CHEMBL251857 94121 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 359 2 1 3 3.6 COc1cc(Br)c2c(c1)NC(=O)C(C)(c1ccccc1)C2=O 10.1016/j.bmcl.2007.11.045
71453361 84003 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2163739 84003 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2219947 84003 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 394 2 1 4 3.7 NC1CCc2c(c3ccccc3n2S(=O)(=O)c2cccc(C(F)(F)F)c2)C1 10.1016/j.bmcl.2012.06.002
136118661 75904 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 75904 0 None -7 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
10314060 168035 0 None -5248 7 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 168035 0 None -5248 7 Human 5.1 pKi = 5.1 Binding
In vitro binding affinity to human 5-hydroxytryptamine 6 receptorIn vitro binding affinity to human 5-hydroxytryptamine 6 receptor
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
155565292 175021 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4579883 175021 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 385 5 0 4 3.0 CCCN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
127026052 137028 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137028 0 None -4 19 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
11258709 130002 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.3 CN(C)CCn1ccc2ccc(NS(=O)(=O)CCc3cccc4ccccc34)cc21 10.1021/jm049615n
CHEMBL368069 130002 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 421 8 1 4 4.3 CN(C)CCn1ccc2ccc(NS(=O)(=O)CCc3cccc4ccccc34)cc21 10.1021/jm049615n
11259180 60230 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 6 1 7 3.7 Cc1cc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL175906 60230 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 437 6 1 7 3.7 Cc1cc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2n1CCN(C)C 10.1021/jm049615n
44401621 68314 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 273 2 1 3 2.7 Nc1ccc(S(=O)(=O)C2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL191972 68314 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperatureBinding affinity against human 5-Hydroxytryptamine 6 receptor expressed in HEK293 cells using [3H]LSD done for 90 minutes at pH 7.4 at room temperature
ChEMBL 273 2 1 3 2.7 Nc1ccc(S(=O)(=O)C2CCc3ccccc32)cc1 10.1016/j.bmcl.2005.02.070
CHEMBL5091373 213791 0 None -354 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 213791 0 None -354 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin)Binding affinity to 5-HT6R (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
168278046 189628 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 401 5 0 5 4.9 COc1cccc(Cn2ccc3c(N4CCC(OC)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5174789 189628 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 401 5 0 5 4.9 COc1cccc(Cn2ccc3c(N4CCC(OC)CC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
49781036 17001 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 797 17 3 9 8.0 Cc1c(S(=O)(=O)Nc2ccc(OCCCCCCCCNS(=O)(=O)c3cccc4c(N(C)C)cccc34)c(N3CCNCC3)c2)sc2ccc(Cl)cc12 10.1021/jm1007177
CHEMBL1256255 17001 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 797 17 3 9 8.0 Cc1c(S(=O)(=O)Nc2ccc(OCCCCCCCCNS(=O)(=O)c3cccc4c(N(C)C)cccc34)c(N3CCNCC3)c2)sc2ccc(Cl)cc12 10.1021/jm1007177
127036186 136889 0 None -23 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 136889 0 None -23 19 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 6 (unknown origin) by competition binding assayBinding affinity to 5-HT 6 (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
135464118 92628 0 None -21 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 92628 0 None -21 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
3117 206106 100 None -5 16 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -5 16 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
134141166 146224 0 None -93 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 496 11 1 5 5.2 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3924375 146224 0 None -93 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 496 11 1 5 5.2 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)NCc3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
90654848 112200 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233673 112200 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3304318 112200 0 None -42 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 484 9 0 4 4.5 CC1(C)C(=O)N(Cc2ccccc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
52912979 127380 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664727 127380 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 377 2 1 5 3.2 Cn1c2c(c3cc(S(=O)(=O)c4ccc(C#N)cc4)ccc31)C1CCC(C2)N1 nan
49781032 16999 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 755 13 2 9 6.5 COc1ccc(N(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1256253 16999 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 755 13 2 9 6.5 COc1ccc(N(CCCCNS(=O)(=O)c2cccc3c(N(C)C)cccc23)S(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1 10.1021/jm1007177
9566 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
95882507 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
CHEMBL4520293 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6Selectivity interaction (GPCR panel (PDSP screen)) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
9566 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
95882507 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
CHEMBL4520293 3371 8 None -1 2 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000353a HTR6
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C nan
851853 190724 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 239 1 1 2 1.5 NC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
CHEMBL5191370 190724 13 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human full length 5HT6R expressed in HEK293 cells by radioligand binding assay
ChEMBL 239 1 1 2 1.5 NC(=O)N1CCN(c2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114319
5 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
5202 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
CHEMBL39 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
DB08839 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990550b
117209965 184665 1 None -3 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 184665 1 None -3 6 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
134 2478 19 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2478 19 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2478 19 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2478 19 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2478 19 None -63 67 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
164620074 185097 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 413 8 2 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCNC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4865076 185097 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 413 8 2 6 2.8 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCNC3)cccc21 10.1016/j.ejmech.2021.113792
24966733 83618 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207383 83618 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2012.10.057
45378936 197825 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
CHEMBL591940 197825 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 448 5 1 6 4.2 CC(C)Cn1nc2ccc(N3CC[C@@H](N)C3)cc2c1S(=O)(=O)c1cccc2ccccc12 10.1021/jm901674f
57391622 71223 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1949970 71223 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
CHEMBL1963100 71223 0 None -11 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]-LSD from human full length cloned 5HT6 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 458 8 1 5 3.8 O=S(=O)(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1cncc2ccccc12 10.1016/j.bmc.2011.12.039
2351 3234 60 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
2820 3234 60 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
5035 3234 60 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
CHEMBL81 3234 60 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
DB00481 3234 60 None -10 21 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O 10.1021/jm2011657
136118658 75901 0 None -8 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 75901 0 None -8 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
162644502 181224 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 348 4 0 3 3.5 O=C1c2ccccc2/C=C\c2ccccc2N1CCCN1CCOCC1 10.1016/j.bmcl.2020.127493
CHEMBL4778076 181224 0 None -3 3 Human 4.1 pKi = 4.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 348 4 0 3 3.5 O=C1c2ccccc2/C=C\c2ccccc2N1CCCN1CCOCC1 10.1016/j.bmcl.2020.127493
137656918 159118 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 372 2 0 5 4.3 N#CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
CHEMBL4103891 159118 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin)
ChEMBL 372 2 0 5 4.3 N#CC1=Cc2cn(S(=O)(=O)c3cccc4ccccc34)c3cccc(c23)O1 10.1021/acsmedchemlett.6b00482
90468604 185962 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 252 1 2 3 2.1 c1ccc2c(c1)nc(N1CCNCC1)c1cc[nH]c12 10.1021/acs.jmedchem.1c00224
CHEMBL4877935 185962 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 252 1 2 3 2.1 c1ccc2c(c1)nc(N1CCNCC1)c1cc[nH]c12 10.1021/acs.jmedchem.1c00224
155561865 175247 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 412 4 2 5 3.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4584746 175247 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 412 4 2 5 3.7 CC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3ccccc3)c3ccc(F)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
2865 4079 67 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 4079 67 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 4079 67 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 4079 67 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 4079 67 None -83 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
155530779 171004 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)c1 10.1016/j.ejmech.2019.111857
CHEMBL4464881 171004 0 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1cccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)c1 10.1016/j.ejmech.2019.111857
45487140 197155 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
CHEMBL583677 197155 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human HT6 receptor expressed in human HeLa cells
ChEMBL 319 4 1 5 2.0 NCCn1cc(S(=O)(=O)c2cccc(F)c2)c2ncccc21 10.1016/j.bmcl.2009.10.067
68115767 131217 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 0 5 3.7 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(C1COC1)CC3 nan
CHEMBL3692958 131217 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 403 3 0 5 3.7 O=S(=O)(c1ccccc1)c1cc(Cl)c2oc3c(c2c1)CN(C1COC1)CC3 nan
54581122 62213 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782367 62213 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 350 2 1 3 4.2 FC(F)(F)c1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
162672516 182540 0 None -14 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
CHEMBL4794963 182540 0 None -14 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 425 8 1 5 5.0 CC(=O)Nc1ccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)cc1 10.1016/j.bmcl.2020.127506
118626101 165171 0 None -251 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4245997 165171 0 None -251 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 489 6 1 5 4.1 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3[nH]ccc23)CC1 10.1016/j.ejmech.2018.01.002
44389024 62947 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 318 5 1 4 3.0 CCCCS(=O)(=O)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
CHEMBL179232 62947 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 318 5 1 4 3.0 CCCCS(=O)(=O)n1cc(C2=CCNCC2)c2ccccc21 10.1016/j.bmcl.2004.10.064
145983144 165327 0 None -7 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4249426 165327 0 None -7 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 520 6 1 4 5.7 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1 10.1016/j.ejmech.2018.01.002
162662778 181410 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 552 10 1 5 6.1 C#CCNC1CCc2c(OCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
CHEMBL4780446 181410 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
ChEMBL 552 10 1 5 6.1 C#CCNC1CCc2c(OCCCN3CCN(c4cccc5c4ccn5Cc4cccc(Cl)c4)CC3)cccc21 10.1016/j.ejmech.2020.112765
11567840 94403 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 413 1 2 3 4.6 CC1(c2ccc(O)c(Br)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253718 94403 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 413 1 2 3 4.6 CC1(c2ccc(O)c(Br)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
168288598 191177 0 None -1949 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 400 10 3 9 1.8 COc1ccccc1N1CCN(CCCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
CHEMBL5197911 191177 0 None -1949 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 400 10 3 9 1.8 COc1ccccc1N1CCN(CCCCCCNc2nc(N)nc(N)n2)CC1 10.1016/j.ejmech.2021.113931
1209 1628 69 None -12 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
203 1628 69 None -12 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
3386 1628 69 None -12 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
CHEMBL41 1628 69 None -12 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
DB00472 1628 69 None -12 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F nan
168287240 191141 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 7 4.4 Nc1nc(NCCOc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
CHEMBL5197266 191141 0 None -1 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 457 9 4 7 4.4 Nc1nc(NCCOc2cccc(Cl)c2Cl)nc(NCCc2c[nH]c3ccccc23)n1 10.1016/j.ejmech.2021.113931
156012823 176836 0 None -29 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 548 11 0 6 6.2 Cc1ccc(S(=O)(=O)N(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2ccccc2)cc1 10.1016/j.bmc.2020.115459
CHEMBL4638388 176836 0 None -29 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 548 11 0 6 6.2 Cc1ccc(S(=O)(=O)N(CCCCCCN2CCN(c3nsc4ccccc34)CC2)c2ccccc2)cc1 10.1016/j.bmc.2020.115459
4976400 173130 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 361 7 2 4 4.7 O=[N+]([O-])c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4535764 173130 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 361 7 2 4 4.7 O=[N+]([O-])c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
145978472 163051 0 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 438 4 1 4 2.7 O=C(c1ccc(Cl)cc1)N1CCN(CCN2CCC3(C2)C(=O)Nc2ccccc23)CC1 10.1016/j.bmcl.2018.06.019
CHEMBL4203581 163051 0 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta scintillation counting analysis
ChEMBL 438 4 1 4 2.7 O=C(c1ccc(Cl)cc1)N1CCN(CCN2CCC3(C2)C(=O)Nc2ccccc23)CC1 10.1016/j.bmcl.2018.06.019
124 2933 44 None -100 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2933 44 None -100 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2933 44 None -100 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2933 44 None -100 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2933 44 None -100 32 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
206 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
68848 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
CHEMBL12314 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
206 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
68848 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
CHEMBL12314 2457 10 None -1318 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm5003759
138691364 171341 2 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 254 3 2 3 2.2 CCn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1016/j.ejmech.2019.03.017
CHEMBL4469847 171341 2 None -1548 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 254 3 2 3 2.2 CCn1cncc1-c1c[nH]c2ccc(C(N)=O)cc12 10.1016/j.ejmech.2019.03.017
155554326 174376 0 None -99 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL4565558 174376 0 None -99 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells
ChEMBL 457 9 0 6 3.2 COc1ccccc1N1CCN(CCCCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
58258770 127438 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ncccc54)ccc31)C1CCC(C2)N1 nan
CHEMBL3664785 127438 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 392 2 1 6 3.1 Cn1c2c(c3cc(S(=O)(=O)n4ccc5ncccc54)ccc31)C1CCC(C2)N1 nan
5 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
5202 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
CHEMBL39 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
DB08839 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(00)00453-4
145 140 48 None -7 29 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
1832 140 48 None -7 29 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
CHEMBL7257 140 48 None -7 29 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
DB14010 140 48 None -7 29 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm990550b
54585045 62208 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
CHEMBL1782362 62208 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 312 3 1 4 3.2 COc1ccc(Sc2ccc3c(c2)N2CCNCC2C3)cc1 10.1016/j.bmcl.2010.07.105
155524885 175647 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4455699 175647 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4594629 175647 0 None 40 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 418 4 1 4 3.9 COc1ccc2c(c1)c(-c1[nH]c3cccc[n+]3c1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
102 4064 44 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
3659 4064 44 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
8969 4064 44 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
CHEMBL15245 4064 44 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
DB01392 4064 44 None -173 49 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 nan
2133793 21617 12 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 476 5 2 5 6.2 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccc(F)cc1 10.1016/j.bmcl.2015.03.049
CHEMBL1319488 21617 12 None -1 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 476 5 2 5 6.2 O=S(=O)(Nc1cc(Sc2cccc3cccnc23)c(O)c2ccccc12)c1ccc(F)cc1 10.1016/j.bmcl.2015.03.049
155532545 171186 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 380 4 2 5 3.2 CC(=O)Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4467359 171186 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 380 4 2 5 3.2 CC(=O)Nc1ncc(-c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
44591069 176143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 461 4 0 6 4.9 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
CHEMBL460002 176143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 461 4 0 6 4.9 O=S(=O)(c1cccc2ccccc12)c1cccc2oc(N3CCN(C4CCCC4)CC3)nc12 10.1016/j.bmcl.2008.12.107
44328589 205960 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCN(C)CC4)cc3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95517 205960 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptorBinding affinity against human 5-hydroxytryptamine 6 receptor
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCN(C)CC4)cc3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10811310 101730 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL302845 101730 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm980532e
10436045 3460 3 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3460 3 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3460 3 None -25 13 Human 7.1 pKi = 7.1 Binding
Binding affinity for 5-hydroxytryptamine 6 receptor was determinedBinding affinity for 5-hydroxytryptamine 6 receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
44398420 67533 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCNCC4)cc3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
CHEMBL191027 67533 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3ncc(N4CCNCC4)cc3c2)sc2ccc(Cl)cc12 10.1021/jm050247c
10811310 101730 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm050247c
CHEMBL302845 101730 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptorBinding affinity for human 5-hydroxytryptamine 6 receptor
ChEMBL 406 6 1 7 2.2 COc1ccc(NS(=O)(=O)c2cccc([N+](=O)[O-])c2)cc1N1CCN(C)CC1 10.1021/jm050247c
134131970 144394 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 487 8 1 5 4.7 CC(=O)Nc1ccc(CCN(C)CC2Cc3ccc4c(ccn4S(=O)(=O)c4ccccc4)c32)cc1 10.1016/j.bmc.2016.10.010
CHEMBL3910287 144394 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 487 8 1 5 4.7 CC(=O)Nc1ccc(CCN(C)CC2Cc3ccc4c(ccn4S(=O)(=O)c4ccccc4)c32)cc1 10.1016/j.bmc.2016.10.010
145973771 164167 0 None -9 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 164167 0 None -9 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
130442480 174698 0 None -97 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -97 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
137631892 155844 0 None -15 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4066426 155844 0 None -15 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 532 6 0 5 5.2 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3ccc(Cl)c(Cl)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
58258864 127416 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 1 6 2.5 Cc1cc(S(=O)(=O)c2cncnc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3664762 127416 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 368 2 1 6 2.5 Cc1cc(S(=O)(=O)c2cncnc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
155556527 173938 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 247 2 1 2 3.3 CCn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4555115 173938 0 None 2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 247 2 1 2 3.3 CCn1cncc1-c1c[nH]c2ccc(F)c(F)c12 10.1016/j.ejmech.2019.03.017
155566925 175291 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 293 1 1 2 3.5 Cn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
CHEMBL4585956 175291 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 293 1 1 2 3.5 Cn1cncc1-c1c[nH]c2ccc(Br)c(F)c12 10.1016/j.ejmech.2019.03.017
10808841 201599 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 365 5 1 7 1.0 COc1ccc(NS(=O)(=O)c2cn(C)cn2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL64715 201599 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSDBinding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD
ChEMBL 365 5 1 7 1.0 COc1ccc(NS(=O)(=O)c2cn(C)cn2)cc1N1CCN(C)CC1 10.1021/jm980532e
49850567 56175 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632217 56175 0 None -3981 9 Human 6.1 pKi = 6.1 Binding
Binding affinity to human recombinant 5-HT6 receptor by radioligand displacement assayBinding affinity to human recombinant 5-HT6 receptor by radioligand displacement assay
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
44439165 145220 0 None -3162 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391661 145220 0 None -3162 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
168295497 191904 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
CHEMBL5209131 191904 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 405 4 0 4 5.5 COC1CCN(c2nc3ccccc3c3c2ccn3Cc2cccc(Cl)c2)CC1 10.1016/j.ejmech.2022.114329
9952250 203252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL76466 203252 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cc(OC)ccc32)cc1 10.1016/s0960-894x(00)00453-4
155555136 173776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cnc2ccccc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4551197 173776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 419 4 1 6 3.8 COc1ccc2c(c1)c(C1=CCNCC1)cn2S(=O)(=O)c1cnc2ccccc2c1 10.1021/acsmedchemlett.6b00056
164612759 184134 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 477 13 2 6 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4850488 184134 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 477 13 2 6 4.4 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
164621427 185208 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 12 2 6 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4866788 185208 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 463 12 2 6 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113783
134130197 141687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 10 1 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884312 141687 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 502 10 1 6 4.6 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134129897 141709 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 11 1 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884704 141709 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 516 11 1 6 5.0 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNCc4ccccc4)CC3)cccc21 10.1016/j.ejmech.2016.08.016
134130069 141724 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 607 10 1 7 6.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
CHEMBL3884858 141724 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counterDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in CHOK1 cell membranes measured after 60 mins by scintillation counter
ChEMBL 607 10 1 7 6.7 O=S(=O)(c1ccccc1)n1ccc2c(N3CCN(CCCCCNc4c5c(nc6ccccc46)CCCC5)CC3)cccc21 10.1016/j.ejmech.2016.08.016
56595406 65311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
CHEMBL1834230 65311 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 328 3 1 3 1.9 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(C)C=N1 10.1021/jm200466r
2870667 93646 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 2 5 3.3 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
CHEMBL249034 93646 9 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 346 5 2 5 3.3 O=[N+]([O-])c1ccc(N2CCNCC2)cc1NCc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.016
11624561 69944 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL187865 69944 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
CHEMBL194307 69944 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 354 4 0 4 3.5 CN1CCC[C@@H]1Cc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1016/j.bmcl.2005.07.028
10202995 70209 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
CHEMBL194786 70209 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 430 5 0 4 5.2 Cc1ccc(S(=O)(=O)n2cc(C3CCN(Cc4ccccc4)C3)c3ccccc32)cc1 10.1016/j.bmcl.2005.07.028
44403096 71784 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
CHEMBL197845 71784 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 390 4 1 6 3.0 Cc1cc(Cl)n(CS(=O)(=O)n2cc(C3=CCCNC3)c3ccccc32)n1 10.1016/j.bmcl.2005.07.028
11524473 134316 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
CHEMBL371886 134316 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 414 6 0 6 3.5 COc1ccc(S(=O)(=O)n2cc(C[C@@H]3CCCN3C)c3ccccc32)cc1OC 10.1016/j.bmcl.2005.07.028
49781038 17544 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 440 6 2 6 3.1 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
CHEMBL1258607 17544 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 440 6 2 6 3.1 COc1ccc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cc1N1CCNCC1 10.1021/jm1007177
155534795 175677 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4471055 175677 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
CHEMBL4594879 175677 0 None 61 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 402 3 2 5 4.3 Cc1nc(N)[nH]c1-c1cn(S(=O)(=O)c2cccc3ccccc23)c2ccccc12 10.1016/j.ejmech.2019.06.001
14571158 148549 1 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
CHEMBL394303 148549 1 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 314 4 1 4 2.7 Cc1ccc(S(=O)(=O)n2cc(CCN)c3ccccc32)cc1 10.1021/jm070521y
127047538 139225 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 482 6 0 7 3.3 COCCS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3798490 139225 0 None 6 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 482 6 0 7 3.3 COCCS(=O)(=O)n1ccc2c(-c3ccc(C(F)(F)F)cc3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
11200157 200078 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
CHEMBL606705 200078 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 391 5 3 3 3.5 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1F 10.1021/jm049243i
11775364 200102 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
CHEMBL606816 200102 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 453 6 2 4 4.5 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm049243i
25122654 198844 0 None 54 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
CHEMBL598851 198844 0 None 54 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor by scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor by scintillation counting
ChEMBL 390 3 2 5 3.0 NC1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc(Cl)c4)c3c2)CC1 10.1021/jm901674f
58258859 123906 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 384 2 1 4 3.8 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3639636 123906 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 384 2 1 4 3.8 Cc1cc(S(=O)(=O)c2cccc(F)c2)cc2c3c(n(C)c12)CC1CCC3N1 nan
20901115 10862 5 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173359 10862 5 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 415 5 1 9 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(NCC1CCCO1)c1sccc12 10.1016/j.bmc.2010.05.051
49836617 18616 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
CHEMBL1278180 18616 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 390 3 1 5 2.8 CN1CCN(c2ccc3[nH]nc(S(=O)(=O)c4ccc(Cl)cc4)c3c2)CC1 10.1021/jm1007825
25263326 183708 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484009 183708 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 316 4 1 3 4.1 Cc1c(C2CCNCC2)ccnc1OCc1cccc(Cl)c1 10.1016/j.bmcl.2009.03.077
16222963 81631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165546 81631 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 466 3 0 4 4.7 CN(C)C1CCc2c(c3cc(Cl)ccc3n2S(=O)(=O)c2ccccc2Br)C1 10.1016/j.bmcl.2012.06.002
58258804 127409 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 372 2 0 5 3.8 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccsc4)cc13)C2 nan
CHEMBL3664755 127409 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 372 2 0 5 3.8 CN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccsc4)cc13)C2 nan
56595534 65317 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
CHEMBL1834238 65317 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 380 4 1 4 3.0 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CCC1c1ccco1 10.1021/jm200466r
52912973 70405 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70405 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
155547259 173091 0 None 21 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4534733 173091 0 None 21 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 357 3 0 4 2.2 CN1CCN(c2cccc3c2CCN3S(=O)(=O)c2ccccc2)CC1 10.1016/j.bmcl.2016.07.055
16222450 81638 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 368 3 0 4 3.6 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
CHEMBL2165553 81638 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 368 3 0 4 3.6 Cc1ccc(S(=O)(=O)n2c3c(c4ccccc42)CC(N(C)C)CC3)cc1 10.1016/j.bmcl.2012.06.002
9885426 116849 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 364 6 0 6 3.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccs1 10.1021/jm010943m
CHEMBL339741 116849 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 364 6 0 6 3.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1cccs1 10.1021/jm010943m
44435623 148465 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL394232 148465 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
25024529 62630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
CHEMBL1785063 62630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 447 4 0 5 3.4 CN1CCN(Cc2ccc3c(ccn3S(=O)(=O)c3ccccc3Br)c2)CC1 10.1021/ml100101u
44435623 148465 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL394232 148465 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 373 4 0 5 3.3 CCN1CCC(n2cc(S(=O)(=O)c3cccc(F)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL5080955 212940 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None O=S(=O)(CC1CCN(CCCc2noc3cc(F)ccc23)C1)c1ccc(F)c(Cl)c1 10.1021/acs.jmedchem.1c00497
CHEMBL5092755 213612 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1ccc(S(=O)(=O)CC2CCN(CCCc3noc4cc(F)ccc34)C2)cc1C 10.1021/acs.jmedchem.1c00497
135398745 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
47 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
CHEMBL715 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
DB00334 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
58230832 176674 2 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 258 1 0 5 1.6 O=S(=O)(Cl)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
CHEMBL4635924 176674 2 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at 5-HT6 receptor (unknown origin)Antagonist activity at 5-HT6 receptor (unknown origin)
ChEMBL 258 1 0 5 1.6 O=S(=O)(Cl)c1c(Cl)nc2n1CCS2 10.1016/j.ejmech.2018.11.017
58258858 127399 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 388 2 1 4 3.6 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)cc(F)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3664745 127399 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 388 2 1 4 3.6 Cn1c2c(c3cc(S(=O)(=O)c4cc(F)cc(F)c4)ccc31)C1CCC(C2)N1 nan
56665086 65355 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
CHEMBL1834340 65355 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 396 4 1 4 4.2 CCN/C(=N\[S+]([O-])c1sc2ccc(Cl)cc2c1C)N1CC(CC)C=N1 10.1021/jm200466r
44403064 133049 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL371132 133049 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1cccc(F)c1)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
44435607 88707 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
CHEMBL236576 88707 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.bmc.2007.06.024
164610136 184352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 398 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCC3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4853545 184352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 398 8 1 5 4.0 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCC3CCCC3)cccc21 10.1016/j.ejmech.2021.113792
44435607 88707 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
CHEMBL236576 88707 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 345 3 1 5 2.5 O=S(=O)(c1ccc(F)cc1)c1cn(C2CCNC2)c2ncccc12 10.1016/j.ejmech.2010.05.045
162651292 179642 0 None -6 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
CHEMBL4749824 179642 0 None -6 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 438 7 1 6 3.3 Cn1ccc2c(S(=O)(=O)N[C@H]3CCN(CCCc4noc5ccccc45)C3)cccc21 10.1016/j.ejmech.2020.112149
24965331 83694 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 477 5 0 6 3.4 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)c(Br)c1 10.1016/j.bmcl.2012.10.057
CHEMBL2207768 83694 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 477 5 0 6 3.4 COc1ccc(S(=O)(=O)n2ccc3c(CN4CCN(C)CC4)cccc32)c(Br)c1 10.1016/j.bmcl.2012.10.057
164627753 185925 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 596 14 2 7 6.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
CHEMBL4877482 185925 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter methodDisplacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
ChEMBL 596 14 2 7 6.9 O=S(=O)(c1ccccc1)n1ccc2c(OCCNCCCCCCNc3c4c(nc5ccccc35)CCCC4)cccc21 10.1016/j.ejmech.2021.113783
23652635 56392 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 411 5 0 5 4.1 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642417 56392 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 411 5 0 5 4.1 CCN1CCN(c2cn(S(=O)(=O)c3ccc(C(C)C)cc3)c3ccccc23)CC1 10.1016/j.bmcl.2010.11.001
68115704 131237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3692978 131237 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 387 4 2 6 3.0 COc1cc(S(=O)(=O)c2ccc([C@H](C)O)cc2)cc2c3c(oc12)CCNC3 nan
59339383 138606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
CHEMBL3787014 138606 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 399 5 2 4 2.3 CCN/C(=N\S(=O)(=O)c1ccc(NC(C)=O)c(Cl)c1)N1CC(CC)C=N1 10.1016/j.bmcl.2016.02.001
10091613 156185 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4070284 156185 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(F)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
47 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
CHEMBL715 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
DB00334 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting methodDisplacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.03.017
137637392 155677 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 6 0 6 3.0 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4064478 155677 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 413 6 0 6 3.0 CCN1CCN(Cc2cn(S(=O)(=O)c3ccccc3)c3ccc(OC)cc23)CC1 10.1021/acs.jmedchem.6b01662
135398745 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
47 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
CHEMBL715 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
DB00334 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.ejmech.2019.06.001
56944665 111618 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290003 111618 0 None -14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 481 8 1 5 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
68115843 131728 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
CHEMBL3696963 131728 0 None - 1 Human 8.1 pKi = 8.1 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 372 2 1 5 3.4 N#Cc1cc(S(=O)(=O)c2ccc(Cl)cc2)cc2c3c(oc12)CCNC3 nan
16222448 81607 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165523 81607 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 354 3 0 4 3.3 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2)C1 10.1016/j.bmcl.2012.06.002
162646653 178922 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
CHEMBL4741142 178922 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 419 7 1 5 3.5 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cccc(Cl)c1 10.1016/j.ejmech.2020.112149
162654406 179998 0 None -22 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4754193 179998 0 None -22 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 459 7 1 6 4.2 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(F)cc2s1 10.1016/j.ejmech.2020.112149
162657622 180555 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
CHEMBL4760655 180555 0 None -3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 469 7 1 5 4.6 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1ccc2cc(Cl)ccc2c1 10.1016/j.ejmech.2020.112149
53327952 111197 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286581 111197 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
58258843 128471 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccn4)c31)C1CCC(C2)N1 nan
CHEMBL3669670 128471 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 459 5 1 6 4.3 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)cc(OCc4ccccn4)c31)C1CCC(C2)N1 nan
49756 202609 9 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 202609 9 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
52899 96805 31 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm030030n
CHEMBL268800 96805 31 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm030030n
137659244 158622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
CHEMBL4098336 158622 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 298 3 1 6 1.1 Cc1ccccc1Cc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2017.04.033
145958329 161782 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
CHEMBL4164725 161782 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 353 4 1 5 3.2 CC(C)c1nc2c(N3CCNCC3)ccnc2n1Cc1ccc(F)cc1 10.1016/j.ejmech.2017.12.053
145949620 162195 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 383 5 1 5 3.9 CC(C)c1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4171417 162195 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 383 5 1 5 3.9 CC(C)c1nc2c(N3CCNCC3)ccnc2n1CCc1cccc(Cl)c1 10.1016/j.ejmech.2017.12.053
2854567 153390 9 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 7 1 6 4.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCCOc3ccc(C(C)(C)C)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL398337 153390 9 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 412 7 1 6 4.1 CN1CCN(c2ccc([N+](=O)[O-])c(NCCOc3ccc(C(C)(C)C)cc3)c2)CC1 10.1016/j.bmcl.2007.09.016
44263496 199840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
CHEMBL605292 199840 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 393 3 1 5 4.5 CC1=CC(C)(C)c2ccc(NS(=O)(=O)c3c(Cl)nc4sccn34)cc21 10.1016/j.bmc.2009.08.006
12017579 98739 8 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(CCN(C)C)c[nH]c2c1 10.1021/jm030030n
CHEMBL281408 98739 8 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(CCN(C)C)c[nH]c2c1 10.1021/jm030030n
156017609 177327 0 None -40 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 464 9 1 6 4.9 O=C1CCc2cc(OCCCCCCN3CCN(c4nsc5ccccc45)CC3)ccc2N1 10.1016/j.bmc.2020.115459
CHEMBL4644906 177327 0 None -40 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 464 9 1 6 4.9 O=C1CCc2cc(OCCCCCCN3CCN(c4nsc5ccccc45)CC3)ccc2N1 10.1016/j.bmc.2020.115459
155540807 171949 0 None -12 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccccc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4483554 171949 0 None -12 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 498 8 2 4 5.2 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccccc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
54584108 62203 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
CHEMBL1782357 62203 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
ChEMBL 296 2 1 3 3.5 Cc1ccccc1Sc1ccc2c(c1)N1CCNCC1C2 10.1016/j.bmcl.2010.07.105
75201901 165872 14 None -602 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None -602 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
90654850 112149 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233674 112149 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302943 112149 0 None -66 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 502 9 0 4 4.6 CC1(C)C(=O)N(Cc2ccc(F)cc2)C(=O)N1CCCCCN1CCN(c2ccc(F)cc2F)CC1 10.1016/j.ejmech.2014.01.065
57403055 70403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cccc(S(=O)(=O)c4ccccc4)c31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950748 70403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cccc(S(=O)(=O)c4ccccc4)c31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
155557523 174093 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 433 4 0 6 4.2 COc1ccc2c(c1)c(C1=CCN(C)CC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
CHEMBL4558840 174093 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 433 4 0 6 4.2 COc1ccc2c(c1)c(C1=CCN(C)CC1)cn2S(=O)(=O)c1ccc2cccnc2c1 10.1021/acsmedchemlett.6b00056
162661549 180820 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
CHEMBL4763622 180820 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 300 3 0 4 2.9 CN(C)c1ccc2c(ccn2S(=O)(=O)c2ccccc2)c1 10.1016/j.ejmech.2020.112916
118626035 164966 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4240954 164966 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2ncccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
23652863 56402 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 5 0 6 3.7 CCN1CCN(c2cn(S(=O)(=O)c3ccc(OC)cc3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642427 56402 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 433 5 0 6 3.7 CCN1CCN(c2cn(S(=O)(=O)c3ccc(OC)cc3)c3cc(Cl)ccc23)CC1 10.1016/j.bmcl.2010.11.001
11575479 94305 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253096 94305 0 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
19779451 93313 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 222 2 1 2 3.3 Nc1ccc(Cn2ccc3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
CHEMBL247281 93313 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 222 2 1 2 3.3 Nc1ccc(Cn2ccc3ccccc32)cc1 10.1016/j.bmcl.2006.12.089
57399090 68079 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmc.2011.09.044
CHEMBL1917342 68079 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting
ChEMBL 440 8 1 6 2.7 COc1ccccc1N1CCN(CCCNS(=O)(=O)c2ccc3ncccc3c2)CC1 10.1016/j.bmc.2011.09.044
3397 203777 104 None -1 2 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
CHEMBL806 203777 104 None -1 2 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 nan
137650961 156791 0 None -50 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
CHEMBL4077538 156791 0 None -50 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta liquid scintillation counting analysis
ChEMBL 482 6 0 5 4.0 O=S(=O)(c1cccc2ncccc12)N1CCC(CCN2CCN(c3cccc(F)c3)CC2)CC1 10.1016/j.bmc.2017.04.046
126720449 161905 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
CHEMBL4166780 161905 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 341 3 1 5 2.9 Cc1nc2c(N3CCNCC3)ccnc2n1Cc1ccccc1Cl 10.1016/j.ejmech.2017.12.053
155541547 172469 0 None 22 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 486 8 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4519004 172469 0 None 22 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 486 8 2 6 5.2 COc1ccc2c(c1)c(-c1[nH]c(NCCc3ccccc3)nc1C)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
155563164 174754 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 4 2 5 3.8 CC(=O)Nc1nc(C)c(-c2c(C)n(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4573880 174754 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 408 4 2 5 3.8 CC(=O)Nc1nc(C)c(-c2c(C)n(S(=O)(=O)c3ccccc3)c3ccccc23)[nH]1 10.1016/j.ejmech.2019.06.001
71151870 117751 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409252 117751 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2ccc(F)cc2)CC1 10.1016/j.ejmech.2014.12.045
57398613 71124 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949759 71124 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962394 71124 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 315 2 1 4 2.4 O=S(=O)(c1ccccc1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
66801167 111617 0 None -165 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
CHEMBL3290002 111617 0 None -165 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 467 7 1 5 4.7 O=S(=O)(NCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cccc2ccccc12 10.1021/jm401895u
74538690 142532 0 None -23 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 511 10 1 4 5.2 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3895172 142532 0 None -23 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 511 10 1 4 5.2 O=C(CCOCCN1CCN(c2ccccc2-c2ccccc2)CC1)NCc1ccc(C(F)(F)F)cc1 10.1016/j.ejmech.2016.05.005
71456780 81007 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 4 3.5 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccc(Cl)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159462 81007 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 426 8 1 4 3.5 O=S(=O)(NCC1CCN(CCOc2cccc(F)c2)CC1)c1cccc(Cl)c1 10.1016/j.ejmech.2012.07.043
44581973 175028 0 None -389 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175028 0 None -389 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in human HeLa cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
162645470 178964 0 None -107 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
CHEMBL4741579 178964 0 None -107 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 minsDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells in presence of serotonin incubated for 60 mins
ChEMBL 536 11 3 7 3.5 COc1cc(N)c(Cl)cc1C(=O)CCC1CCN(CCNS(=O)(=O)c2ccc(NC(C)=O)cc2)CC1 10.1016/j.ejmech.2016.05.048
118736372 118439 0 None -13 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 7 0 9 2.6 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
CHEMBL3423336 118439 0 None -13 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 7 0 9 2.6 Cc1cn2c3c(=O)n(C)c(=O)n(C)c3nc2n1CCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.ejmech.2015.04.046
168281850 190443 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.3 Clc1cccc(Cn2ccc3c(NCC4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
CHEMBL5187034 190443 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 391 5 1 4 5.3 Clc1cccc(Cn2ccc3c(NCC4CCOC4)nc4ccccc4c32)c1 10.1016/j.ejmech.2022.114329
164616670 184030 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4849077 184030 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 424 7 1 7 3.8 CCCCC(Oc1cc(Cl)cc(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
118736397 118446 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 511 7 0 10 1.7 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423379 118446 0 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 511 7 0 10 1.7 Cn1c(=O)c2c(nc3n(CCCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
71463516 84872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 329 5 0 5 2.4 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccncc12 10.1007/s00044-004-0121-8
CHEMBL2260374 84872 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cellsDisplacement of [3H]LSD from Homo sapiens (human) 5-HT6 receptor expressed in Homo sapiens (human) HEK293 cells
ChEMBL 329 5 0 5 2.4 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccncc12 10.1007/s00044-004-0121-8
5 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 66 None -169 54 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptorDisplacement of [3H]LSD from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
90656159 110341 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 321 3 1 3 2.6 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
CHEMBL3260791 110341 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 321 3 1 3 2.6 O=C1CC(c2ccccc2)CN1c1cccc(N2CCNCC2)c1 10.1016/j.bmcl.2014.03.049
50878551 90314 60 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90314 60 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
66800991 111576 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 8 2.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289963 111576 0 None -13 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 456 7 1 8 2.4 O=S(=O)(NCCCN1CCN(c2nsc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
142601333 185181 0 None -36 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4866412 185181 0 None -36 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5HT6 receptor (unknown origin)Binding affinity to 5HT6 receptor (unknown origin)
ChEMBL 260 2 2 3 2.0 Fc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
44404396 71113 0 None -45 5 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196169 71113 0 None -45 5 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT6 receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
134153716 151952 0 None -70 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3971125 151952 0 None -70 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 510 11 1 5 5.8 COc1ccc(-c2ccccc2N2CCN(CCCCCC(=O)N[C@H](C)c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11849789 165617 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1ccc(N2CCNCC2)cc1)c1ccccc1 10.1021/jm060469q
CHEMBL426332 165617 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assayBinding affinity to human 5HT6 receptor in HEK293 cells by radioligand binding assay
ChEMBL 317 4 2 4 1.9 O=S(=O)(Nc1ccc(N2CCNCC2)cc1)c1ccccc1 10.1021/jm060469q
44568065 190492 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 4 0 5 3.7 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C(C)C)CC3)c1 10.1016/j.bmcl.2008.06.030
CHEMBL518762 190492 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 398 4 0 5 3.7 COc1cccc(S(=O)(=O)n2c3c(c4ccccc42)CCN(C(C)C)CC3)c1 10.1016/j.bmcl.2008.06.030
155562519 174640 0 None -17 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccc(F)cc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
CHEMBL4571321 174640 0 None -17 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method
ChEMBL 516 8 2 4 5.3 COc1ccc2[nH]cc(C3CC(=O)N(CCCCN4CCC(c5c[nH]c6ccc(F)cc56)CC4)C3=O)c2c1 10.1016/j.ejmech.2019.111736
57391618 71125 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1949763 71125 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
CHEMBL1962395 71125 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 333 2 1 4 2.5 O=S(=O)(c1cccc(F)c1)c1ccc2c(c1)O[C@H]1CNCC[C@@H]21 10.1016/j.bmcl.2011.12.026
57403835 71127 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1949767 71127 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
CHEMBL1962397 71127 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 345 3 1 5 2.4 COc1cccc(S(=O)(=O)c2ccc3c(c2)O[C@H]2CNCC[C@@H]32)c1 10.1016/j.bmcl.2011.12.026
50878551 90314 60 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90314 60 None -2 18 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
11407151 61284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2n1CCN(C)C 10.1021/jm049615n
CHEMBL177119 61284 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 407 6 1 4 4.5 Cc1cc2cc(NS(=O)(=O)c3ccc4ccccc4c3)ccc2n1CCN(C)C 10.1021/jm049615n
10028436 3476 3 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3476 3 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3476 3 None -426 12 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
6075 149575 36 None -13 16 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
CHEMBL395110 149575 36 None -13 16 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 nan
156015769 177005 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 388 4 1 5 2.8 COc1cc2c3c(c1OC)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
CHEMBL4640588 177005 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method
ChEMBL 388 4 1 5 2.8 COc1cc2c3c(c1OC)-c1cc(NS(C)(=O)=O)ccc1CC3N(C)CC2 10.1016/j.bmc.2020.115578
164615243 184627 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4857676 184627 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 5 1 7 3.0 CCC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
118736396 118445 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 6 0 10 1.3 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
CHEMBL3423378 118445 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells incubated for 60 mins by microbeta plate reader based method
ChEMBL 497 6 0 10 1.3 Cn1c(=O)c2c(nc3n(CCCCN4CCN(c5ccc(Cl)cc5)CC4)c(=O)ccn23)n(C)c1=O 10.1016/j.ejmech.2015.04.046
136118649 75969 0 None -9 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058704 75969 0 None -9 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
90654840 112137 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3233669 112137 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
CHEMBL3302757 112137 0 None -323 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 478 10 0 5 4.2 COc1ccccc1N1CCN(CCCCCN2C(=O)N(Cc3ccccc3)C(=O)C2(C)C)CC1 10.1016/j.ejmech.2014.01.065
145990586 166290 0 None -67 11 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166290 0 None -67 11 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT6 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
55479093 81009 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 366 7 1 5 2.6 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
CHEMBL2159464 81009 1 None -10 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 366 7 1 5 2.6 O=S(=O)(NC1CCN(CCOc2ccccc2)CC1)c1cccs1 10.1016/j.ejmech.2012.07.043
2291 3135 52 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3135 52 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3135 52 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3135 52 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3135 52 None -12 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
155562918 174611 0 None 5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4570584 174611 0 None 5 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 314 4 1 7 1.1 Cc1ccccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
127045870 139558 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 416 5 0 8 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3cnn(C)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
CHEMBL3800576 139558 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting methodDisplacement of [3H]LSD from human 5HT6 receptor in HEK293 cell membrane incubated for 1 hr by scintillation counting method
ChEMBL 416 5 0 8 2.0 CC(C)CS(=O)(=O)n1ccc2c(-c3cnn(C)c3)cc(N3CCN(C)CC3)nc21 10.1016/j.bmcl.2016.04.024
90656169 110351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 338 3 1 4 3.1 COc1ccccc1C1CN(c2ccc3c(c2)CCNCC3)C(=O)O1 10.1016/j.bmcl.2014.03.049
CHEMBL3260802 110351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 338 3 1 4 3.1 COc1ccccc1C1CN(c2ccc3c(c2)CCNCC3)C(=O)O1 10.1016/j.bmcl.2014.03.049
56944664 111581 0 None -79 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
CHEMBL3289968 111581 0 None -79 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 428 8 1 6 3.0 Cc1cccc(S(=O)(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm401895u
7185124 10851 2 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
CHEMBL1173210 10851 2 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assayBinding affinity to human recombinant 5HT6 receptor expressed in HEK293 cells by radioligand displacement assay
ChEMBL 385 3 0 8 2.8 O=S(=O)(c1ccccc1)c1nnn2c1nc(N1CCCC1)c1sccc12 10.1016/j.bmc.2010.05.051
846090 169022 9 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 286 7 1 5 2.3 Cc1cc(OCCN(C)C)nc(NCc2ccccc2)n1 10.1016/j.ejmech.2019.111857
CHEMBL4436098 169022 9 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 286 7 1 5 2.3 Cc1cc(OCCN(C)C)nc(NCc2ccccc2)n1 10.1016/j.ejmech.2019.111857
44397258 13693 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1195611 13693 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL554985 13693 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 0 2 2.7 CN1CCC[C@H]1Cn1ccc2ccccc21 10.1016/j.bmcl.2005.05.092
135476741 154985 9 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL404232 154985 9 None -14 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cellsDisplacement of [3H]LSD from human recombinant 5HT6 receptor stably expressed in HEK cells
ChEMBL 254 1 2 2 1.8 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccccc23)C1=O 10.1016/j.bmc.2013.09.011
11631738 94214 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 1 1 2 4.7 CC1(c2ccc(Cl)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL252496 94214 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 353 1 1 2 4.7 CC1(c2ccc(Cl)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
122483275 137582 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 137582 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 137582 0 None -39 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT6 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
107 141 116 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
1833 141 116 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
CHEMBL8165 141 116 None -66 30 Human 7.1 pKi = 7.1 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm990550b
137651282 156913 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccccc3F)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4079150 156913 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 302 3 1 6 0.9 CN1CCN(c2nc(N)nc(Cc3ccccc3F)n2)CC1 10.1016/j.ejmech.2017.04.033
45484332 195455 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 373 5 0 5 3.1 O=S(=O)(c1cccc(F)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
CHEMBL567805 195455 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 373 5 0 5 3.1 O=S(=O)(c1cccc(F)c1)c1cn(CCN2CCCC2)c2ncccc12 10.1016/j.bmc.2009.05.055
49836507 18561 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
CHEMBL1277835 18561 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 372 4 2 6 1.8 COc1ccc(S(=O)(=O)c2n[nH]c3cccc(N4CCNCC4)c23)cc1 10.1021/jm1007825
24784578 176142 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 4.7 CCCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL460001 176142 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 449 6 0 6 4.7 CCCCN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
16023081 59662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 356 3 1 5 2.6 COc1cc(OC)cc(N2C(=O)CSC23C(=O)Nc2ccccc23)c1 10.1016/j.bmcl.2014.03.049
CHEMBL1733660 59662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cell membrane after 3 hrs by liquid scintillation counting analysis
ChEMBL 356 3 1 5 2.6 COc1cc(OC)cc(N2C(=O)CSC23C(=O)Nc2ccccc23)c1 10.1016/j.bmcl.2014.03.049
71727067 90835 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401937 90835 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3217036 90835 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 414 5 0 5 4.3 COc1ccc2c(=O)c3cc(CN4CCN(Cc5ccccc5)CC4)ccc3oc2c1 10.1016/j.bmcl.2013.05.062
25251903 174646 11 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 334 4 0 5 3.2 CN1CCN(c2ccnc(SCc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.111857
CHEMBL4571369 174646 11 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 334 4 0 5 3.2 CN1CCN(c2ccnc(SCc3ccccc3Cl)n2)CC1 10.1016/j.ejmech.2019.111857
49756 202609 9 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm010943m
CHEMBL7143 202609 9 None 2 8 Human 7.1 pKi = 7.1 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm010943m
44568019 183329 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1cccc(C(F)(F)F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
CHEMBL481278 183329 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HeLa cells
ChEMBL 394 2 1 4 3.6 O=S(=O)(c1cccc(C(F)(F)F)c1)n1c2c(c3ccccc31)CCNCC2 10.1016/j.bmcl.2008.06.030
242 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
34 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
60795 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL1112 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
DB01238 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2018.01.002
CHEMBL5076846 212693 0 None -138 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None C[C@H]1C[C@H](NS(=O)(=O)c2cc3ccc(F)cc3s2)CN1CCCc1noc2cc(F)ccc12 10.1021/acs.jmedchem.1c00497
44446214 94488 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL254331 94488 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 349 2 1 3 4.1 COc1ccc([C@@]2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
2883218 174244 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 350 5 1 4 4.8 Oc1c(CN2CCCC2)cc(CSc2ccccc2)c2cccnc12 10.1016/j.ejmech.2019.111857
CHEMBL4562431 174244 1 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibitory constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibitory constant
ChEMBL 350 5 1 4 4.8 Oc1c(CN2CCCC2)cc(CSc2ccccc2)c2cccnc12 10.1016/j.ejmech.2019.111857
13069626 120093 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3361000 120093 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
CHEMBL3546103 120093 0 None -8912 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 440 8 0 9 1.4 COc1ccccc1N1CCN(CCCCCn2cnc3c2c(=O)n(C)c(=O)n3C)CC1 10.1016/j.bmc.2014.11.008
9923440 113679 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 327 8 2 4 2.9 OCCCNC[C@H]1CCc2ccc(OCc3ccccc3)cc2O1 10.1021/jm5003952
CHEMBL3329448 113679 0 None - 1 Human 8.1 pKi = 8.1 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 327 8 2 4 2.9 OCCCNC[C@H]1CCc2ccc(OCc3ccccc3)cc2O1 10.1021/jm5003952
58258795 128493 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
CHEMBL3669692 128493 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 418 3 1 6 3.5 Cn1c2c(c3cc(S(=O)(=O)c4cccc(-n5cccn5)c4)ccc31)C1CCC(C2)N1 nan
129892069 192139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assayDisplacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assay
ChEMBL 428 6 1 5 4.2 CN(C)CCn1cnc2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc21 10.1016/j.bmcl.2021.128275
CHEMBL5220504 192139 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assayDisplacement of [3H] LSD from human 5-HT6R expressed in HEK293 cell membrane assessed as inhibition constant by competition binding assay
ChEMBL 428 6 1 5 4.2 CN(C)CCn1cnc2ccc(NS(=O)(=O)c3ccc4c(Cl)cccc4c3)cc21 10.1016/j.bmcl.2021.128275
155563374 174674 0 None 131 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
CHEMBL4572158 174674 0 None 131 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells by microbeta liquid scintillation counting
ChEMBL 423 3 1 5 4.5 O=S(=O)(c1ccc2cccnc2c1)n1cc(C2=CCNCC2)c2cc(Cl)ccc21 10.1021/acsmedchemlett.6b00056
25131339 180441 0 None 26 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4759208 180441 0 None 26 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 355 3 0 5 2.6 CN1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
118626121 164868 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238479 164868 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cccc2cnccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
10117854 126903 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL366012 126903 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 500 5 0 5 5.7 O=S(=O)(c1ccc(Br)s1)n1cc(C2CCN(Cc3ccccc3)C2)c2ccccc21 10.1016/j.bmcl.2005.07.028
53327952 111197 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
CHEMBL3286581 111197 0 None 31 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 353 2 1 5 2.2 O=S(=O)(c1ccccc1)n1cc2c3c(cccc31)N1CCNCC1C2 10.1021/jm5003759
164623922 185583 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 456 8 1 5 5.2 O=S(=O)(c1cccc2ccccc12)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
CHEMBL4872486 185583 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysisDisplacement of [3H]LSD from human 5HT6 receptor expressed in CHO-K1 membrane incubated for 60 mins by solid scintillation counting analysis
ChEMBL 456 8 1 5 5.2 O=S(=O)(c1cccc2ccccc12)n1ccc2c(OCCNCc3ccccc3)cccc21 10.1016/j.ejmech.2021.113792
155531362 171061 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 456 6 2 6 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc(F)c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
CHEMBL4465638 171061 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 456 6 2 6 4.1 CCC(=O)Nc1nc(C)c(-c2cn(S(=O)(=O)c3cccc(F)c3)c3ccc(OC)cc23)[nH]1 10.1016/j.ejmech.2019.06.001
155568300 175800 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4590882 175800 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4595815 175800 0 None 794 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 386 4 2 6 3.0 COc1ccc2c(c1)c(-c1cnc(N)[nH]1)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155555526 175830 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4552168 175830 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
CHEMBL4596003 175830 0 None 125 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 400 4 2 6 3.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1cccc(F)c1 10.1016/j.ejmech.2019.06.001
155521504 176021 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4451939 176021 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
CHEMBL4597600 176021 0 None 117 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 432 4 2 6 4.3 COc1ccc2c(c1)c(-c1[nH]c(N)nc1C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.ejmech.2019.06.001
45484299 195541 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
CHEMBL568249 195541 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells
ChEMBL 397 5 0 5 3.7 CN(C)CCn1cc(S(=O)(=O)c2c(Cl)cccc2Cl)c2cccnc21 10.1016/j.bmc.2009.05.055
155555238 173758 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
CHEMBL4550806 173758 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in CHO-K1 cells incubated for 3 hrs by scintillation counting analysis
ChEMBL 356 3 0 3 3.2 CN1CCC(c2cccc3c2CN(S(=O)(=O)c2ccccc2)C3)CC1 10.1016/j.bmcl.2016.07.055
11154032 200609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 407 5 3 3 4.1 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1Cl 10.1021/jm049243i
CHEMBL610255 200609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 407 5 3 3 4.1 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccc(F)cc1Cl 10.1021/jm049243i
11201726 200613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
CHEMBL610259 200613 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 447 5 2 3 4.4 CN1CCC[C@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc12 10.1021/jm049243i
44397650 13652 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL1195348 13652 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
CHEMBL554369 13652 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 214 2 1 1 2.8 CN1CCC[C@H]1Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2005.05.092
162651619 179731 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
CHEMBL4751063 179731 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 7 1 6 4.7 O=S(=O)(N[C@@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccc(Cl)cc2s1 10.1016/j.ejmech.2020.112149
71462330 81634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Cl)C1 10.1016/j.bmcl.2012.06.002
CHEMBL2165549 81634 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HEK293 cells
ChEMBL 388 3 0 4 4.0 CN(C)C1CCc2c(c3ccccc3n2S(=O)(=O)c2ccccc2Cl)C1 10.1016/j.bmcl.2012.06.002
58258791 128469 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669668 128469 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 426 6 1 6 3.4 COCCOc1cc(S(=O)(=O)c2ccccc2)cc2c3c(n(C)c12)CC1CCC3N1 nan
66800947 157688 0 None -9 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4088249 157688 0 None -9 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 433 6 2 3 4.0 O=S(=O)(NCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
137638969 156329 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3c(Cl)cccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4071816 156329 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3c(Cl)cccc32)cc1 10.1021/acs.jmedchem.6b01662
137644304 157509 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4085949 157509 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 465 4 0 5 3.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(F)cc23)CC1 10.1021/acs.jmedchem.6b01662
44403059 123854 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL363827 123854 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 356 3 1 4 3.4 O=S(=O)(c1ccccc1F)n1cc(C2=CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
11574663 154570 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 390 4 1 3 4.9 CCN(CC)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
CHEMBL401970 154570 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 390 4 1 3 4.9 CCN(CC)c1ccc(C2(C)C(=O)Nc3cc(Cl)cc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2007.11.045
23652787 56394 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
CHEMBL1642419 56394 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assayDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay
ChEMBL 451 3 0 5 3.5 CN1CCN(c2cn(S(=O)(=O)c3ccc(F)cc3)c3ccc(Br)cc23)CC1 10.1016/j.bmcl.2010.11.001
58258827 127434 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 467 3 1 5 5.3 Cn1c2c(c3cc(S(=O)(=O)c4cn(-c5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
CHEMBL3664781 127434 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 467 3 1 5 5.3 Cn1c2c(c3cc(S(=O)(=O)c4cn(-c5ccccc5)c5ccccc45)ccc31)C1CCC(C2)N1 nan
20042470 13799 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL1196366 13799 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
CHEMBL556759 13799 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against 5 Hydroxy tryptamine 6 receptorBinding affinity against 5 Hydroxy tryptamine 6 receptor
ChEMBL 288 2 1 2 3.9 c1ccc(-c2cc(N3CCNCC3)c3ccccc3c2)cc1 10.1016/j.bmcl.2005.01.031
56595531 65315 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
CHEMBL1834235 65315 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 390 4 1 3 3.4 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1N=CC[C@H]1c1ccccc1 10.1021/jm200466r
25263308 183657 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
CHEMBL483560 183657 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 318 4 1 3 3.3 Cc1c(OCc2ccc(F)c(F)c2)cccc1N1CCNCC1 10.1016/j.bmcl.2009.03.077
10203612 61295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 439 8 2 3 5.2 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cc(Cl)cc(Cl)c3)cc12 10.1021/jm049615n
CHEMBL177124 61295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 439 8 2 3 5.2 CCN(CC)CCc1c[nH]c2ccc(NS(=O)(=O)c3cc(Cl)cc(Cl)c3)cc12 10.1021/jm049615n
68108369 131147 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 6 3.1 O=S(=O)(c1ccccc1)c1cc(-n2cccn2)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692888 131147 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 379 3 1 6 3.1 O=S(=O)(c1ccccc1)c1cc(-n2cccn2)c2oc3c(c2c1)CNCC3 nan
25024726 62640 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(Cl)cc2)CC1 10.1021/ml100101u
CHEMBL1785073 62640 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 437 4 0 5 3.9 CN1CCN(Cc2ccc3c(c2)c(Cl)cn3S(=O)(=O)c2ccc(Cl)cc2)CC1 10.1021/ml100101u
44435644 88700 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
CHEMBL236571 88700 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT6 receptorBinding affinity to 5HT6 receptor
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.ejmech.2010.05.045
44386408 62678 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 5 0 5 4.2 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
CHEMBL178691 62678 0 None - 1 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cellsAbility to displace [3H]LSD from human 5-hydroxytryptamine 6 receptor transiently expressed in COS-7 cells
ChEMBL 412 5 0 5 4.2 COc1ccc2c(c1)c1c(n2S(=O)(=O)c2ccc(C)cc2)CCCC1CN(C)C 10.1016/j.bmcl.2004.01.071
44435644 88700 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
CHEMBL236571 88700 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5HT6 expressed in HeLa cells
ChEMBL 461 4 0 5 4.7 CC(C)N1CCCC(n2cc(S(=O)(=O)c3cccc(Br)c3)c3cccnc32)C1 10.1016/j.bmc.2007.06.024
12017573 162892 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3ccc(OC)cc32)c1 10.1016/s0960-894x(00)00453-4
CHEMBL419824 162892 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 418 8 0 7 3.0 COc1ccc(OC)c(S(=O)(=O)n2cc(CCN(C)C)c3ccc(OC)cc32)c1 10.1016/s0960-894x(00)00453-4
135398737 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 944 89 None -4 91 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
16116900 59785 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1642847 59785 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
CHEMBL1739252 59785 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 420 5 3 5 4.0 O=S(=O)(c1cccc2ccccc12)c1n[nH]c2cccc(NCC3CCNCC3)c12 10.1016/j.bmc.2010.10.033
68115752 131750 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 0 4 3.8 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
CHEMBL3696985 131750 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 389 2 0 4 3.8 CC(=O)N1CCc2oc3c(Cl)cc(S(=O)(=O)c4ccccc4)cc3c2C1 nan
58258841 128489 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
CHEMBL3669688 128489 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.Binding Assay: The relative affinities of the various compounds for the 5-HT6 receptor were measured in a radioligand binding assay, using a sintillation proximity assay (SPA) format.
ChEMBL 433 3 1 6 3.9 COc1cc(S(=O)(=O)c2cncc3ccccc23)cc2c3c(n(C)c12)CC1CCC3N1 nan
10091389 157658 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
CHEMBL4087957 157658 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 383 4 0 5 2.9 Cc1ccc(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)cc1 10.1021/acs.jmedchem.6b01662
46880657 6302 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
CHEMBL1082198 6302 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 362 3 1 4 3.3 O=S(=O)(c1cccc(F)c1)c1cn(C2CCNC2)c2ccc(F)cc12 10.1016/j.bmcl.2010.01.073
52912973 70405 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
CHEMBL1950750 70405 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 352 2 1 4 3.4 Cn1c2c(c3cc(S(=O)(=O)c4ccccc4)ccc31)C1CCC(C2)N1 10.1016/j.bmcl.2012.01.022
24763349 62301 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783608 62301 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 405 3 1 4 4.4 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4ccc5ccccc5c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
135339817 180902 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 180902 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting methodDisplacement of [3H]lysergic acid diethylamide from human recombinant 5HT6 receptor stably expressed in CHO cell membranes measured after 30 mins by liquid scintillation counting method
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
11316967 129232 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 453 4 2 3 5.6 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5c(Cl)cccc45)cc23)CC1 10.1021/jm049615n
CHEMBL367481 129232 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 453 4 2 3 5.6 CN1CCC(c2c[nH]c3ccc(NS(=O)(=O)c4cccc5c(Cl)cccc45)cc23)CC1 10.1021/jm049615n
24783809 176139 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
CHEMBL459988 176139 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells
ChEMBL 407 3 0 6 3.6 CN1CCN(c2nc3c(S(=O)(=O)c4cccc5ccccc45)cccc3o2)CC1 10.1016/j.bmcl.2008.12.107
162654006 179908 0 None -39 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
CHEMBL4753094 179908 0 None -39 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in CHOK1 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 425 7 1 6 3.6 O=S(=O)(N[C@H]1CCN(CCCc2noc3ccccc23)C1)c1cc2ccccc2o1 10.1016/j.ejmech.2020.112149
11236269 128783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
CHEMBL367088 128783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm5003952
9953284 203088 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm010943m
CHEMBL75010 203088 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
ChEMBL 408 6 0 5 4.1 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccc2ccccc2c1 10.1021/jm010943m
16116898 59812 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1642877 59812 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
CHEMBL1739545 59812 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 434 4 3 5 3.5 O=C(Nc1cccc2c(S(=O)(=O)c3cccc4ccccc34)n[nH]c12)C1CCCNC1 10.1016/j.bmc.2010.10.033
16117282 59822 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642888 59822 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739615 59822 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cellsDisplacement of [3H]-LSD from cloned human 5-HT6 receptor expressed in human HeLa cells
ChEMBL 386 5 3 6 2.6 COc1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
44403046 134737 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 3 1 5 3.4 O=S(=O)(c1cccs1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
CHEMBL372569 134737 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL 346 3 1 5 3.4 O=S(=O)(c1cccs1)n1cc(C2CCCNC2)c2ccccc21 10.1016/j.bmcl.2005.07.028
57398803 69399 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1935589 69399 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
CHEMBL1949758 69399 0 None -3 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from full length rat 5HT6 receptorDisplacement of [3H]LSD from full length rat 5HT6 receptor
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CNCC3 10.1016/j.bmcl.2011.11.050
11236269 128783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
CHEMBL367088 128783 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 449 6 1 7 3.9 O=S(=O)(Nc1ccc2c(ccn2CCN2CCCC2)c1)c1c(Cl)nc2sccn12 10.1021/jm049615n
68108586 123940 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCNC3 nan
CHEMBL3639917 123940 0 None - 1 Human 8.0 pKi = 8.0 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 313 2 1 4 2.9 O=S(=O)(c1ccccc1)c1ccc2c3c(oc2c1)CCNC3 nan
24965680 83606 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207371 83606 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 4 0 5 2.8 CN1CCN(Cc2cccc3c2ccn3S(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2012.10.057
44397322 12149 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL1184645 12149 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
CHEMBL361892 12149 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cellsBinding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
ChEMBL 304 4 0 2 4.3 CN1CCC[C@@H]1Cn1cc(Cc2ccccc2)c2ccccc21 10.1016/j.bmcl.2005.05.092
71151683 117750 0 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(F)c2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409251 117750 0 None 4 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 486 9 1 5 4.5 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3Cc2cccc(F)c2)CC1 10.1016/j.ejmech.2014.12.045
68115694 131197 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1cc(F)cc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
CHEMBL3692938 131197 0 None - 1 Human 8.0 pKi = 8 Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL 383 2 1 4 3.8 O=S(=O)(c1cc(F)cc(F)c1)c1cc(Cl)c2oc3c(c2c1)CNCC3 nan
23955921 109252 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 413 8 1 5 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
CHEMBL322980 109252 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
ChEMBL 413 8 1 5 3.7 CCN(CC)CCc1cn(S(=O)(=O)c2ccc(NC(C)=O)cc2)c2ccccc12 10.1016/s0960-894x(03)00612-7
155541866 172480 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4519266 172480 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 376 8 2 4 4.8 COc1ccc(-c2ccc(CNCCc3c[nH]c4ccc(OC)cc34)o2)cc1 10.1016/j.ejmech.2019.111857
242 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
34 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
60795 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
CHEMBL1112 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
DB01238 467 117 None -144 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2012.11.042
52945114 16990 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 776 17 4 9 6.2 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNC(=O)CCCCC2SC[C@@H]3NC(=O)N[C@H]23)CC1 10.1021/jm1007177
CHEMBL1256172 16990 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 776 17 4 9 6.2 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(CCCCCCNC(=O)CCCCC2SC[C@@H]3NC(=O)N[C@H]23)CC1 10.1021/jm1007177
24777062 94253 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
CHEMBL252774 94253 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 330 4 1 3 2.9 CN(C)[C@H]1CCc2c(cccc2NS(=O)(=O)c2ccccc2)C1 10.1021/jm070910s
24776941 94353 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 5 0 3 4.3 CN(C)CCc1cn(Sc2ccccc2)c2ccccc12 10.1021/jm070910s
CHEMBL253397 94353 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 296 5 0 3 4.3 CN(C)CCc1cn(Sc2ccccc2)c2ccccc12 10.1021/jm070910s
11259419 197000 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 1 5 5.2 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
CHEMBL579981 197000 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 447 6 1 5 5.2 Cc1c(S(=O)(=O)Nc2ccc3ccn(CCN(C)C)c3c2)sc2ccc(Cl)cc12 10.1021/jm049615n
137634238 156111 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 394 4 0 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(C#N)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4069360 156111 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 394 4 0 6 2.5 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(C#N)cc3)c3ccccc23)CC1 10.1021/acs.jmedchem.6b01662
24966738 83616 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207381 83616 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 481 4 0 5 4.0 CN1CCN(Cc2cccc3c2c(Cl)cn3S(=O)(=O)c2ccccc2Br)CC1 10.1016/j.bmcl.2012.10.057
145954503 161869 0 None 7 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 370 5 1 4 4.1 O[C@H](CCN1CCc2onc(-c3ccc(F)c(F)c3)c2C1)c1ccccc1 10.1016/j.ejmech.2018.04.010
CHEMBL4166092 161869 0 None 7 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta TopCount analysis
ChEMBL 370 5 1 4 4.1 O[C@H](CCN1CCc2onc(-c3ccc(F)c(F)c3)c2C1)c1ccccc1 10.1016/j.ejmech.2018.04.010
71574206 85841 0 None -39 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 512 7 1 5 4.7 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312641 85841 0 None -39 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hrDisplacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 after 1 hr
ChEMBL 512 7 1 5 4.7 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccc(Cl)cc2c1 10.1016/j.ejmech.2012.11.042
176 394 63 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -5 31 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
164618482 185333 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4868911 185333 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)c(Cl)c3)n2)CC1 10.1016/j.ejmech.2020.112529
1534 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
71458650 81019 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cccc(Cl)c2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159474 81019 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 454 7 1 5 4.1 O=S(=O)(NC1CCN(CCOc2cccc(Cl)c2Cl)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
4723431 170857 13 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 316 6 2 2 4.8 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
CHEMBL4462814 170857 13 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis
ChEMBL 316 6 2 2 4.8 c1ccc(-c2ccc(CNCCc3c[nH]c4ccccc34)o2)cc1 10.1016/j.ejmech.2019.111857
137633849 156079 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(OC)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
CHEMBL4069104 156079 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 6 0 7 2.6 COc1ccc(OC)c(S(=O)(=O)n2cc(CN3CCN(C)CC3)c3ccccc32)c1 10.1021/acs.jmedchem.6b01662
10246639 5984 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCNCC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
CHEMBL1080574 5984 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrsDisplacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 2 hrs
ChEMBL 340 3 1 4 3.4 O=S(=O)(c1ccccc1)c1cn(C2CCNCC2)c2ccccc12 10.1016/j.bmcl.2010.01.073
57399547 70407 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 0 4 4.1 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
CHEMBL1950752 70407 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assayDisplacement of [3H]LSD from human 5-HT6 serotonin receptor by scintillation proximity assay
ChEMBL 380 3 0 4 4.1 CCN1C2CCC1c1c(n(C)c3ccc(S(=O)(=O)c4ccccc4)cc13)C2 10.1016/j.bmcl.2012.01.022
155558408 174183 0 None 4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(Cl)ccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
CHEMBL4560883 174183 0 None 4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R expressed in human HEK293 cells incubated for 1 hr by radioligand binding assay
ChEMBL 348 4 1 7 1.7 Cc1cc(Cl)ccc1OCc1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2019.06.022
1534 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102566 51 None -8 12 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
118724647 120094 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3361004 120094 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
CHEMBL3546104 120094 0 None -53 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells
ChEMBL 381 6 0 7 1.7 Cn1c(=O)c2c(ncn2CCCCCN2CCc3ccccc3C2)n(C)c1=O 10.1016/j.bmc.2014.11.008
155552213 176084 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4546775 176084 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4598090 176084 0 None -9 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 481 8 0 3 6.5 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2019.06.028
56944952 156825 0 None -26 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
CHEMBL4077937 156825 0 None -26 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting
ChEMBL 447 7 2 3 4.4 O=S(=O)(NCCCN1CC=C(c2c[nH]c3ccc(Cl)cc23)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.7b00839
145985505 165073 0 None -30 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4243579 165073 0 None -30 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 491 6 0 7 3.7 O=S(=O)(c1cccc2cnccc12)N1CCC[C@H]1CCN1CCN(c2noc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
126720407 162276 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 365 5 1 6 3.0 COc1cccc(Cn2c(C(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
CHEMBL4172620 162276 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method
ChEMBL 365 5 1 6 3.0 COc1cccc(Cn2c(C(C)C)nc3c(N4CCNCC4)ccnc32)c1 10.1016/j.ejmech.2017.12.053
24855831 65304 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 404 5 1 3 3.5 CCC1C=NN(/C(=N/S(=O)(=O)c2ccccc2Cl)NCc2ccccc2)C1 10.1021/jm200466r
CHEMBL1834222 65304 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 404 5 1 3 3.5 CCC1C=NN(/C(=N/S(=O)(=O)c2ccccc2Cl)NCc2ccccc2)C1 10.1021/jm200466r
56593935 65365 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 378 5 1 3 2.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CF)(CF)C=N1 10.1021/jm200466r
CHEMBL1834351 65365 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation countingDisplacement of [3H]-methyllysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting
ChEMBL 378 5 1 3 2.2 CCN/C(=N\S(=O)(=O)c1cccc(Cl)c1)N1CC(CF)(CF)C=N1 10.1021/jm200466r
25263316 183830 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 295 4 1 2 4.3 Cc1cccc(COc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
CHEMBL484608 183830 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptorDisplacement of [3H]LSD from human recombinant 5HT6 receptor
ChEMBL 295 4 1 2 4.3 Cc1cccc(COc2cccc(C3CCNCC3)c2C)c1 10.1016/j.bmcl.2009.03.077
134131976 144442 0 None -34 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 509 10 1 5 5.2 N#Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccc(F)cc3-c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
CHEMBL3910730 144442 0 None -34 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting analysis
ChEMBL 509 10 1 5 5.2 N#Cc1ccc(CNC(=O)CCCCCN2CCN(c3ccc(F)cc3-c3ccc(C#N)cc3)CC2)cc1 10.1016/j.ejmech.2016.05.005
11603453 154751 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 7 1 4 4.6 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
CHEMBL402923 154751 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from 5HT6 receptor expressed in HEK293 cells
ChEMBL 387 7 1 4 4.6 CN1CCN(c2ccc(OCc3ccccc3)c(NCc3ccccc3)c2)CC1 10.1016/j.bmcl.2007.09.016
12017575 203032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)cc1 10.1016/s0960-894x(00)00453-4
CHEMBL74378 203032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligandBinding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand
ChEMBL 388 7 0 6 3.0 COc1ccc(S(=O)(=O)n2cc(CCN(C)C)c3cccc(OC)c32)cc1 10.1016/s0960-894x(00)00453-4
155563827 175866 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4572629 175866 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
CHEMBL4596298 175866 0 None 13 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method
ChEMBL 422 4 1 7 3.9 COc1ccc2c(c1)c(-c1nc3n(c1C)CCCN3)cn2S(=O)(=O)c1ccccc1 10.1016/j.ejmech.2019.06.001
24763351 62293 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
CHEMBL1783600 62293 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells
ChEMBL 373 3 1 4 3.3 CN1CCC(c2n[nH]c3ccc(S(=O)(=O)c4cccc(F)c4)cc23)CC1 10.1016/j.bmcl.2009.04.108
5 139 66 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 66 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 66 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 66 None -169 54 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT6 receptorDisplacement of radiolabeled serotonin from human 5HT6 receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
164620109 185145 0 None -54 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 466 8 0 6 4.4 CN1CCN(Cc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
CHEMBL4865907 185145 0 None -54 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to 5-HT6 receptor (unknown origin)Binding affinity to 5-HT6 receptor (unknown origin)
ChEMBL 466 8 0 6 4.4 CN1CCN(Cc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2)CC1 10.1016/j.bmcl.2021.127909
168291659 191440 0 None -131 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
CHEMBL5202120 191440 0 None -131 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysisDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis
ChEMBL 356 8 3 8 1.4 Nc1nc(N)nc(NCCCCCN2CCN(c3ccccc3)CC2)n1 10.1016/j.ejmech.2021.113931
71727065 101936 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL2401931 101936 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
CHEMBL3039720 101936 0 None -389 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 430 5 0 6 4.3 COc1ccc2c(=O)c3cccc(CN4CCN(c5ccccc5OC)CC4)c3oc2c1 10.1016/j.bmcl.2013.05.062
155530351 175710 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4464370 175710 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
CHEMBL4595115 175710 0 None 1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader methodDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cell membranes after 1 hr by microbeta plate reader method
ChEMBL 517 8 0 4 5.8 O=S1(=O)c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmc.2019.06.028
44438723 151040 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 5 0 4 3.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
CHEMBL396329 151040 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H] LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 5 0 4 3.6 CN(C)CCc1cn(S(=O)(=O)c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.12.089
11417978 63344 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
CHEMBL180110 63344 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 393 6 1 4 4.2 CN(C)CCn1ccc2cc(NS(=O)(=O)c3cccc4ccccc34)ccc21 10.1021/jm049615n
145985718 164973 0 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4241081 164973 0 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 521 6 0 7 4.6 O=S(=O)(c1cccc2ncccc12)N1CCCC[C@@H]1CCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2018.01.002
121238069 158580 0 None 79 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
CHEMBL4097856 158580 0 None 79 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cellsDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells
ChEMBL 284 3 1 6 0.8 CN1CCN(c2nc(N)nc(Cc3ccccc3)n2)CC1 10.1016/j.ejmech.2017.04.033
137630619 160535 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4094296 160535 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
CHEMBL4116784 160535 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 434 4 1 6 2.4 O=S(=O)(c1ccccc1Br)n1cc(CN2CCNCC2)c2ncccc21 10.1021/acs.jmedchem.6b01662
164615340 184847 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
CHEMBL4861431 184847 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 382 4 1 7 2.7 CC(Oc1ccc(Cl)c(Cl)c1)c1nc(N)nc(N2CCN(C)CC2)n1 10.1016/j.ejmech.2020.112529
56944189 111601 0 None -16 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 454 8 1 8 2.4 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
CHEMBL3289987 111601 0 None -16 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysisDisplacement of [3H]LSDm from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting analysis
ChEMBL 454 8 1 8 2.4 O=S(=O)(NCCCCN1CCN(c2noc3ccccc23)CC1)c1cnc2ccccn12 10.1021/jm401895u
53327953 111199 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286583 111199 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
71455001 81027 0 None -4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 7 1 4 2.5 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
CHEMBL2159482 81027 0 None -4 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 400 7 1 4 2.5 O=S(=O)(NC1CCN(CCOc2cccc(F)c2)C1)c1ccc(F)c(F)c1 10.1016/j.ejmech.2012.07.043
155533028 171230 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 458 9 0 5 5.1 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4468036 171230 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 458 9 0 5 5.1 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmcl.2019.06.029
11683768 94301 1 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 1 1 2 4.7 CC1(c2ccc(I)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253061 94301 1 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 1 1 2 4.7 CC1(c2ccc(I)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
71449642 81021 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 7 1 5 2.8 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
CHEMBL2159476 81021 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 386 7 1 5 2.8 O=S(=O)(NC1CCN(CCOc2ccccc2)C1)c1ccc(Cl)s1 10.1016/j.ejmech.2012.07.043
10450930 81606 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 356 4 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)c1n2S(=O)(=O)c2ccccc2-1 10.1016/j.bmcl.2012.06.002
CHEMBL2165522 81606 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5-HT6 receptorBinding affinity to human 5-HT6 receptor
ChEMBL 356 4 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)c1n2S(=O)(=O)c2ccccc2-1 10.1016/j.bmcl.2012.06.002
71456783 81025 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 418 7 1 4 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
CHEMBL2159480 81025 0 None -6 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr
ChEMBL 418 7 1 4 3.1 O=S(=O)(NC1CCN(CCOc2cccc3c2CCCC3)C1)c1ccc(F)cc1 10.1016/j.ejmech.2012.07.043
53327953 111199 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
CHEMBL3286583 111199 1 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysisDisplacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis
ChEMBL 367 2 1 5 2.5 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)N2CCNCC2C3)cc1 10.1021/jm5003759
137644129 157618 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 545 6 0 6 4.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(OCC(F)(F)F)cc23)CC1 10.1021/acs.jmedchem.6b01662
CHEMBL4087429 157618 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-LSD from recombinant human 5-HT6 receptor expressed in HEK293 cells after 60 mins
ChEMBL 545 6 0 6 4.3 CN1CCN(Cc2cn(S(=O)(=O)c3ccc(Br)cc3)c3ccc(OCC(F)(F)F)cc23)CC1 10.1021/acs.jmedchem.6b01662
86288949 112128 0 None -1318 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3233665 112128 0 None -1318 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
CHEMBL3302599 112128 0 None -1318 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysisDisplacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
ChEMBL 434 8 0 4 3.8 CN1C(=O)N(CCCCCN2CCN(c3ccccc3)CC2)C(C)(c2ccccc2)C1=O 10.1016/j.ejmech.2014.01.065
168299277 192094 0 None -281 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 404 8 0 5 4.2 CCOCC(Oc1c(C)cccc1Cl)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219333 192094 0 None -281 2 Human 5.0 pKi = 5.0 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 404 8 0 5 4.2 CCOCC(Oc1c(C)cccc1Cl)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
2872937 117425 6 None 2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 464 4 1 5 4.7 O=S(=O)(Nc1cc2c(c3ccccc13)OC1(N3CCOCC3)CCCCC21)c1ccccc1 10.1016/j.bmcl.2015.03.049
CHEMBL3403332 117425 6 None 2 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uMDisplacement of [3H]LSD from human cloned 5-HT6R expressed in HEK293 cells at 0.1 and 1 uM
ChEMBL 464 4 1 5 4.7 O=S(=O)(Nc1cc2c(c3ccccc13)OC1(N3CCOCC3)CCCCC21)c1ccccc1 10.1016/j.bmcl.2015.03.049
162672560 182600 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4795614 182600 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2ccc3ccn(S(=O)(=O)c4ccccc4)c3c2)CC1 10.1016/j.ejmech.2020.112916
162676389 182798 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
CHEMBL4797942 182798 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor incubated for 1 hr by microbeta counting method
ChEMBL 383 3 0 5 2.5 CC(=O)N1CCN(c2cn(S(=O)(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.ejmech.2020.112916
127033666 138442 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3785278 138442 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 364 4 1 4 2.2 CCN/C(=N\S(=O)(=O)c1cccc(OC)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
58158748 138563 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
CHEMBL3786563 138563 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-N-Methyl-Lysergic acid diethylamide from human 5-HT6 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 349 3 2 4 1.8 CCN/C(=N\S(=O)(=O)c1cccc(N)c1)N1CC2(C=N1)CCCC2 10.1016/j.bmcl.2016.02.001
11476494 78536 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 8 1 7 4.1 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
CHEMBL2112986 78536 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cellsInhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
ChEMBL 451 8 1 7 4.1 CCN(CC)CCn1ccc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc21 10.1021/jm049615n
24966734 83619 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 497 4 0 5 4.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL2207384 83619 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 497 4 0 5 4.5 CN1CCN(Cc2cccc3c2c(Br)cn3S(=O)(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2012.10.057
CHEMBL5079536 212850 0 None -14 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]-LSD from human 5-HT6 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
ChEMBL None None None Cc1c(S(=O)(=O)N[C@H]2C[C@H](C)N(CCCc3noc4cc(F)ccc34)C2)sc2ccc(Cl)cc12 10.1021/acs.jmedchem.1c00497
152215 96550 46 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL26655 96550 46 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
10315621 65799 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2c(F)cccc21 10.1016/j.bmcl.2004.09.003
CHEMBL184066 65799 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cellsBinding affinity against human 5-hydroxytryptamine 6 receptor transfected in HeLa cells
ChEMBL 346 5 0 4 3.2 CN(C)CCn1cc(S(=O)(=O)c2ccccc2)c2c(F)cccc21 10.1016/j.bmcl.2004.09.003
52899 96805 31 None 7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm990550b
CHEMBL268800 96805 31 None 7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligandBinding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm990550b
44405257 72656 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 4 1 8 2.3 Nc1ccc(S(=O)(=O)n2ccc3c([N+](=O)[O-])cc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2005.08.059
CHEMBL200844 72656 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells
ChEMBL 362 4 1 8 2.3 Nc1ccc(S(=O)(=O)n2ccc3c([N+](=O)[O-])cc([N+](=O)[O-])cc32)cc1 10.1016/j.bmcl.2005.08.059
118712403 113658 0 None - 1 Human 7.0 pKi = 7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 320 2 1 3 3.8 O=C(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
CHEMBL3329427 113658 0 None - 1 Human 7.0 pKi = 7 Binding
Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cellsAntagonist activity at human recombinant 5HT6 receptor expressed in CHO cells
ChEMBL 320 2 1 3 3.8 O=C(c1ccccc1)n1cc(C2=CCNCC2)c2cc(F)ccc21 10.1021/jm5003952
23288143 159371 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 316 2 0 3 4.0 CN1CC=C(c2cn(C(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
CHEMBL410710 159371 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSDBinding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
ChEMBL 316 2 0 3 4.0 CN1CC=C(c2cn(C(=O)c3ccccc3)c3ccccc23)CC1 10.1016/j.bmcl.2004.10.064
24968181 83613 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
CHEMBL2207378 83613 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cellsDisplacement of [3H]-LSD from cloned human 5HT6 receptor expressed in HEK293 cells
ChEMBL 445 5 0 5 4.4 CC(C)c1ccc(S(=O)(=O)n2cc(Cl)c3c(CN4CCN(C)CC4)cccc32)cc1 10.1016/j.bmcl.2012.10.057
44435219 91360 0 None -30 4 Human 5.0 pKi = 5 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL241115 91360 0 None -30 4 Human 5.0 pKi = 5 Binding
Antagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT6 receptor (unknown origin) by PDSP assay
ChEMBL 367 2 0 2 6.2 O=C(Cc1ccc2ccccc2c1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
168276831 189546 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 369 3 0 4 4.5 c1ccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)cc1 10.1016/j.ejmech.2022.114329
CHEMBL5173511 189546 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assayDisplacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
ChEMBL 369 3 0 4 4.5 c1ccc(Cn2ccc3c(N4CCC5(COC5)C4)nc4ccccc4c32)cc1 10.1016/j.ejmech.2022.114329
118626088 164849 0 None -199 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4238124 164849 0 None -199 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting methodDisplacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL 508 6 0 7 3.4 O=S(=O)(c1cccc2ncccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2018.01.002
168298474 192117 0 None -245 3 Human 5.0 pKi = 5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 384 8 0 5 3.9 CCOCC(Oc1c(C)cccc1C)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
CHEMBL5219968 192117 0 None -245 3 Human 5.0 pKi = 5 Binding
Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constantBinding affinity to 5-HT6R (unknown origin) assessed as inhibition constant
ChEMBL 384 8 0 5 3.9 CCOCC(Oc1c(C)cccc1C)N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2021.128275
155526651 170608 0 None -45 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
CHEMBL4458938 170608 0 None -45 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting methodDisplacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
ChEMBL 464 8 0 4 5.7 O=C1c2cccc3cccc(c23)N1CCCCCCN1CCN(c2cccc3cccnc23)CC1 10.1016/j.bmcl.2019.06.029
164622318 185254 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
CHEMBL4867534 185254 0 None 1 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting methodDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
ChEMBL 396 6 1 7 2.5 CN1CCN(c2nc(N)nc(CCCOc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2020.112529
5 139 66 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5202 139 66 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
CHEMBL39 139 66 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
DB08839 139 66 None -125 54 Rat 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
275 3308 6 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3308 6 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3308 6 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3308 6 None -1 2 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
4106 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 3H-5HT -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5HT -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5HT -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5HT -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5HT -7 33 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1238 201484 21 3H-LSD -3 16 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 3H-LSD -3 16 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
4106 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -1 33 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 3H-LSD -4 33 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -4 33 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -4 33 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -4 33 Mouse 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1809 134 28 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -218 36 Mouse 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4106 2466 16 3H-LSD -7 33 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -7 33 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -7 33 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -7 33 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 4089 56 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
103 4089 56 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -3 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -1 53 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
None 214166 0 125I-LSD 7 10 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
46780481 107045 18 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-LSD -8 53 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
4106 2466 16 3H-LSD -1 33 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -1 33 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -1 33 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -1 33 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 3H-LSD -7 33 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -7 33 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -7 33 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -7 33 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1238 201484 21 3H-LSD -5 16 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 3H-LSD -5 16 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
4106 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1621 2396 16 3H-LSD -17 44 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -17 44 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -17 44 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -17 44 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -17 44 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
4106 2466 16 125I-LSD -4 33 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 125I-LSD -4 33 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 125I-LSD -4 33 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 125I-LSD -4 33 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135398737 944 89 3H-LSD -4 91 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -4 65 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10257 728 28 3H-5HT -39 18 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 728 28 3H-5HT -39 18 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 728 28 3H-5HT -39 18 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 728 28 3H-5HT -39 18 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
282 1391 0 3H-5HT -1122 7 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1391 0 3H-5HT -1122 7 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135 2496 38 3H-5HT -9 57 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-5HT -9 57 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-5HT -9 57 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-5HT -9 57 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-5HT -9 57 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
6450478 214238 0 3H-LSD -1 11 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
1524 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 125I-LSD -457 51 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1830 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
188 3339 73 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
196968 3339 73 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
CHEMBL473186 3339 73 UNDEFINED -3162 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C None
54841 201437 51 3H-5HT -1 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 201437 51 3H-5HT -1 28 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 214629 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
3075702 215594 0 3H-LSD -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1220 186 46 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 186 46 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-LSD -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 125I-LSD -7943 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
11957541 1430 38 3H-5HT -1819 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1430 38 3H-5HT -1819 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1430 38 3H-5HT -1819 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1430 38 3H-5HT -1819 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1430 38 3H-5HT -1819 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
681 1437 65 3H-5HT -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-5HT -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-5HT -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-5HT -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-5HT -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
107780 1814 50 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1814 50 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1814 50 3H-LSD -3162 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1524 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 125I-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-LSD -7244 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
484 2814 45 3H-5HT -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-5HT -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-5HT -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-LSD -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
127 3078 45 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3078 45 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3078 45 3H-5HT -22908 15 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
119570 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-LSD -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
165193 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 3H-5HT -10000 42 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
243 3153 85 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3153 85 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3153 85 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3153 85 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3153 85 3H-5HT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
274 3287 39 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3287 39 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3287 39 3H-LSD -331 3 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
2402 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 3H-LSD -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 3H-LSD -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
6917970 3635 54 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3635 54 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3635 54 3H-LSD -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
2543 3651 66 3H-LSD -218 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3651 66 3H-LSD -194 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-LSD -218 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-LSD -194 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-LSD -218 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-LSD -194 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-LSD -218 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-LSD -194 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-LSD -218 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-LSD -194 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
213 3792 50 3H-LSD -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 3H-LSD -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 3H-LSD -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 3H-LSD -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 3H-LSD -549 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2662 11279 124 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11279 124 3H-LSD -41 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10297 26905 29 3H-LSD -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-LSD -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46537 95 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
54477 84230 34 3H-5HT -138 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-5HT -138 22 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
21830793 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 93798 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93798 96 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 99505 79 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99505 79 3H-LSD -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
446220 132998 13 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-LSD -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167228 22 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
5280343 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 3H-LSD -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
12016890 190182 4 3H-5HT -16982 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190182 4 3H-5HT -16982 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
54676228 192874 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192874 108 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 194860 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194860 87 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198867 110 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-LSD -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 201336 85 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201336 85 3H-LSD -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201790 12 3H-LSD -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 202981 15 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-LSD -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 203133 4 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203133 4 3H-LSD -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 203630 21 3H-LSD -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 203790 64 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203790 64 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203790 64 3H-LSD -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
6852400 214160 0 3H-5HT -25118 21 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-5HT -25118 21 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
None 214217 0 3H-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
None 214236 0 3H-5HT - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 2 1 2.1 C[N+](C)(C)CCC1=CNC2=C1C=C(C=C2)O None
None 214236 0 3H-LSD - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 2 1 2.1 C[N+](C)(C)CCC1=CNC2=C1C=C(C=C2)O None
None 214237 0 125I-LSD -436 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 2 1 6 2.4 CN1C2CCC1CC(C2)OC(=O)N3C4=C(C=CC(=C4)OC)NC3=O.Cl None
104911 214249 0 3H-LSD -41686 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 214360 0 3H-Lysergic -2754 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 C1COC(C2=CC=CC=C21)CCN3CCN(CC3)C4=CC=C(C=C4)S(=O)(=O)N None
25137849 214425 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-LSD -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214461 0 3H-LSD -933 15 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
None 214486 0 3H-LSD -95499 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
3821 214549 0 3H-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214560 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-LSD -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-LSD -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-LSD -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214567 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214574 0 3H-LSD -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-LSD -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214576 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 214577 0 3H-LSD -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 214578 0 3H-LSD -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214579 0 3H-LSD -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214580 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 214639 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214640 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214641 0 3H-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
3672 214642 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)CC1=CC=C(C=C1)C(C)C(=O)O None
84003 214643 0 3H-LSD -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 214644 0 3H-LSD -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214645 0 3H-LSD -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
5090 214646 0 3H-LSD -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
119607 214647 0 3H-LSD -97 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
None 214648 0 3H-LSD -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 214747 0 3H-LSD -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1830 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-LSD -13 27 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1342 36 42 125I-2-iodo LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 36 42 125I-LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 125I-2-iodo LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 125I-LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 125I-2-iodo LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 125I-LSD -45 18 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 125I-LSD -42 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
11954224 214174 0 3H-5HT -181 59 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1353 1880 85 3H-LSD -1047 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
265 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
135398737 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 UNDEFINED -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
122265 1944 0 3H-LSD - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
273 1944 0 3H-LSD - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
CHEMBL1191534 1944 0 3H-LSD - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C None
135398737 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135409468 2004 63 3H-LSD -4 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-LSD -4 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-LSD -4 40 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
265 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 125I-LSD 4 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
2389 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
10257 728 28 3H-LSD -8 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 728 28 3H-LSD -8 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 728 28 3H-LSD -8 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 728 28 3H-LSD -8 18 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
2389 3279 114 3H-LSD -616 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -616 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -616 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -616 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -616 67 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
214 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-LSD -81 29 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 [3H]lysergic acid diethylamide -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 [3H]lysergic acid diethylamide -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 [3H]lysergic acid diethylamide -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 [3H]lysergic acid diethylamide -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 [3H]lysergic acid diethylamide -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2726 906 64 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -10 72 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 214174 0 3H- LSD -141 59 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214174 0 3H-LSD -141 59 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
5 139 66 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -125 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
134 2478 19 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-5HT -10 67 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
135398737 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 125I-LSD -4 91 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1342 36 42 3H-LSD -45 18 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 36 42 3H-LSD -45 18 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 36 42 3H-LSD -45 18 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
135 2496 38 3H-5HT -22 57 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-5HT -22 57 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-5HT -22 57 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-5HT -22 57 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-5HT -22 57 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
31101 720 39 3H-5HT -181 35 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-5HT -181 35 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-5HT -181 35 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-5HT -181 35 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-5HT -181 35 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
None 214168 0 3H-5HT -89 23 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
15387 214209 0 3H-LSD -186 23 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
3652 4034 72 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4034 72 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4034 72 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4034 72 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4034 72 3H-LSD -30 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
15387 214209 0 3H-LSD -186 23 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CC1)CCCC(=O)C2=CC=C(C=C2)F None
2389 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 116 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-LSD -35 30 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2337 3205 72 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -144 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 2869 108 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 214161 0 125I-LSD -141 20 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 214161 0 125I-LSD -141 20 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
5 139 66 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -169 54 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
277 1274 55 125I-LSD -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
277 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 125I-LSD -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 125I-LSD -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 125I-LSD -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 125I-LSD -93 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
277 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 125I-LSD -58 45 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
179 396 107 3H-LSD -134 50 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-LSD -134 50 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-LSD -134 50 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-LSD -134 50 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-LSD -134 50 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
1225 1443 24 125I-LSD -478 21 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 125I-LSD -478 21 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 125I-LSD -478 21 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 125I-LSD -478 21 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 125I-LSD -478 21 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135398737 944 89 3H-LSD -4 91 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3294 1975 106 3H-LSD -87 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -87 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -87 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -87 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -87 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2337 3205 72 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 UNDEFINED -54 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
180 397 50 3H-LSD -99 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -99 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -99 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -99 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -99 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
214 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2274 3124 53 3H-LSD -23 32 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 3H-LSD -23 32 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 3H-LSD -23 32 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 3H-LSD -23 32 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 3H-LSD -23 32 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4543 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
1150 3817 116 3H-LSD -20 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3817 116 3H-LSD -20 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3817 116 3H-LSD -20 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3817 116 3H-LSD -20 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
2274 3124 53 3H-LSD -70 32 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 3H-LSD -70 32 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 3H-LSD -70 32 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 3H-LSD -70 32 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 3H-LSD -70 32 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4543 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 125I-LSD -20 29 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
1613 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5074 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1212 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1613 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -5 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
209 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
277 1274 55 3H-LSD -93 45 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-LSD -93 45 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-LSD -93 45 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-LSD -93 45 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-LSD -93 45 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
16106 117643 28 3H-LSD -3 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 3H-LSD -3 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
5 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -125 54 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1150 3817 116 3H-5HT -20 24 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3817 116 3H-5HT -20 24 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3817 116 3H-5HT -20 24 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3817 116 3H-5HT -20 24 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
240 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 931 39 3H-5HT -316 25 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
107780 1814 50 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1814 50 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1814 50 3H-LSD -3162 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
206 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
2389 3279 114 3H-LSD -2454 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2470 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1712 2456 0 3H-LSD -39 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-LSD -39 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-LSD -39 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-LSD -39 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-LSD -39 21 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2470 3596 46 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-LSD -7413 59 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-LSD -7413 59 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5074 3280 75 3H-5HT -69 29 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-5HT -69 29 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-5HT -69 29 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-5HT -69 29 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-5HT -97 29 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
16351 102257 41 3H-LSD -7 5 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL304902 102257 41 3H-LSD -7 5 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
279 1631 26 3H-LSD -3 17 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 3H-LSD -3 17 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 3H-LSD -3 17 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
1621 2396 16 3H-5HT -17 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-5HT -17 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-5HT -17 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-5HT -17 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-5HT -17 44 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
209 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
73333 5886 23 3H-LSD -1 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5886 23 3H-LSD -1 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
242 467 117 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -40 51 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
282 1391 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1391 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
242 467 117 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
282 1391 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
522609 1391 0 125I-LSD -1819 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 577 5 3 6 2.5 CC(CC1C(=O)N2CCCC2C2(N1C(=O)C(O2)(NC(=O)C1CN(C)C2C(C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135398737 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -26 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
209 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
209 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-LSD -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-LSD -19 23 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
10090005 214210 0 3H-LSD -6 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
1238 201484 21 3H-LSD -3 16 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 3H-LSD -3 16 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
214 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-LSD -81 29 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
206 2457 10 125I-LSD -1318 24 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2457 10 125I-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 125I-LSD -1318 24 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 125I-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 125I-LSD -1318 24 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 125I-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 3H-LSD -1995 24 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
7153 97570 74 3H-LSD -91 33 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97570 74 3H-LSD -91 33 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1209 1628 69 125I-LSD -46 31 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 125I-LSD -46 31 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 125I-LSD -46 31 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 125I-LSD -46 31 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 125I-LSD -46 31 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2337 3205 72 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
107 141 116 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -66 30 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
134 2478 19 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -63 67 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
180 397 50 3H-LSD -154 38 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -154 38 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -154 38 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -154 38 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -154 38 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3294 1975 106 3H-LSD -87 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -87 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -87 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -87 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -87 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1809 134 28 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -6918 36 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2337 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2726 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135 2496 38 125I-LSD -9 57 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 125I-LSD -9 57 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 125I-LSD -9 57 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 125I-LSD -9 57 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 125I-LSD -9 57 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1427 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-5HT -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
152 361 18 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 361 18 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 361 18 125I-LSD -263 18 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2389 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2543 3651 66 3H-5HT -954 31 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-5HT -954 31 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-5HT -954 31 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-5HT -954 31 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-5HT -954 31 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4106 2466 16 3H-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-LSD -7 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1621 2396 16 3H-LSD -16 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -16 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -16 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -16 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -16 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3533 78 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-LSD -9 48 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
11954224 214174 0 3H-LSD -181 59 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398745 2869 108 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-Risperidone -4 65 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1238 201484 21 3H-LSD -5 16 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 3H-LSD -5 16 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2396 16 3H-LSD -17 44 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -17 44 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -17 44 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -17 44 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -17 44 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1621 2396 16 3H-LSD -9 44 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -9 44 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -9 44 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -9 44 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -9 44 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
135398737 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-5HT -4 91 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2865 4079 67 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2726 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -10 72 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2389 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 UNDEFINED -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11954259 214201 0 3H-LSD -870 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
11954259 214201 0 3H-LSD -870 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
1427 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 125I-LSD -19 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
130 3444 43 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3444 43 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3444 43 35S-GTPGammaS -588 13 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
242 467 117 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
107 141 116 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-LSD -35 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2389 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 116 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-LSD -13 30 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
7153 97570 74 125I-LSD -125 33 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97570 74 125I-LSD -125 33 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5 139 66 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -125 54 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
185 3943 54 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-LSD -10715 37 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2389 3279 114 3H-LSD -2454 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115237 55296 113 3H-LSD -89 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-LSD -89 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
206 2457 10 3H-5HT -16 24 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 3H-5HT -16 24 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 3H-5HT -16 24 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1220 186 46 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-5HT -199 44 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3036864 201066 16 125I-LSD -10471 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 125I-LSD -10471 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 125I-LSD -10471 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 125I-LSD -10471 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
7153 97570 74 UNDEFINED -125 33 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97570 74 UNDEFINED -125 33 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1809 134 28 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 28 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -6918 36 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-5HT -6918 36 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
134 2478 19 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -147 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3651 66 3H-LSD -218 31 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-LSD -218 31 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-LSD -218 31 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-LSD -218 31 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-LSD -218 31 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
133 2460 48 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5HT -87 42 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1613 2316 44 3H-LSD -4 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -4 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -4 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -4 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -4 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398745 2869 108 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
186 1777 47 3H-LSD -363 16 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1777 47 3H-LSD -363 16 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1777 47 3H-LSD -363 16 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
5656 201377 82 3H-5HT 3 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201377 82 3H-5HT 3 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1212 1632 45 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -48 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
274 3287 39 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3287 39 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3287 39 3H-LSD 1 3 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
1524 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-LSD -257 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
279 1631 26 3H-LSD -7 17 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 3H-LSD -7 17 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 3H-LSD -7 17 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
4106 2466 16 3H-5HT -7 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5HT -7 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5HT -7 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5HT -7 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2105 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
265 128 0 3H-LSD 4 2 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 3H-LSD 4 2 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 3H-LSD 4 2 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
11653679 180609 1 UNDEFINED -44 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 180609 1 UNDEFINED -44 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
11976 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
11976 907 54 3H-LSD -3 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-LSD -3 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-LSD -3 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-LSD -3 23 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
11976 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-LSD -2 23 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135 2496 38 3H-LSD -9 57 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -9 57 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -9 57 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -9 57 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -9 57 Mouse 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
107 141 116 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -35 30 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2726 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
133 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 2478 19 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -63 67 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1588 2294 24 3H-5HT -41 43 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-5HT -41 43 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-5HT -41 43 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-5HT -41 43 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-5HT -41 43 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
133 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 125I-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2105 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 125I-LSD -31 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1613 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
191 399 92 125I-LSD -7 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 125I-LSD -7 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 125I-LSD -7 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 125I-LSD -7 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 125I-LSD -7 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
135398737 944 89 3H-5HT -4 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-5HT -4 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-5HT -4 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-5HT -4 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-5HT -4 91 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1346 83 108 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
280 83 108 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
9899402 83 108 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
CHEMBL9666 83 108 125I-LSD -2570 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
37459 735 10 3H-5HT -74 24 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-5HT -74 24 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-5HT -74 24 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 944 89 125I-LSD -8 91 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 125I-LSD -8 91 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 125I-LSD -8 91 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 125I-LSD -8 91 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 125I-LSD -8 91 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
133 2460 48 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2460 48 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5HT -58 42 Mouse 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-LSD -87 42 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
5074 3280 75 3H-5HT -97 29 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-5HT -97 29 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-5HT -97 29 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-5HT -97 29 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
28 3440 37 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3440 37 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3440 37 3H-LSD -1905 10 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1613 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
11954259 214201 0 3H-LSD -870 43 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
31101 720 39 3H-LSD -23 35 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-LSD -23 35 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-LSD -23 35 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-LSD -23 35 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-LSD -23 35 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1613 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-LSD -4 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3205 72 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5074 3280 75 3H-LSD -97 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-LSD -97 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-LSD -97 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-LSD -97 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
180 397 50 3H-5HT -154 38 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-5HT -154 38 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-5HT -154 38 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-5HT -154 38 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-5HT -154 38 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
134 2478 19 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-5HT -147 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1809 134 28 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-LSD -6918 36 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
145 140 48 3H-LSD -7 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-LSD -7 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-LSD -7 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-LSD -7 29 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
270 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
6918447 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
CHEMBL80937 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
270 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
6918447 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
CHEMBL80937 2262 0 125I-LSD - 1 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl None
173 3211 88 3H-LSD -41 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3211 88 3H-LSD -41 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3211 88 3H-LSD -41 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1353 1880 85 3H-LSD -1047 85 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-LSD -2951 85 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -2951 85 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -2951 85 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -2951 85 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -2951 85 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
134 2478 19 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2478 19 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 125I-LSD -63 67 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 125I-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1212 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
135 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-5HT -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1212 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-LSD -48 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
107 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1712 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1712 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 3H-LSD -12 21 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
206 2457 10 3H-LSD -1318 24 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 3H-LSD -1318 24 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 3H-LSD -1318 24 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
None 214366 0 3H-LSD -3890 23 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
107 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 125I-LSD -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 139 66 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 125I-LSD -63 54 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
135398737 944 89 3H-5HT -8 91 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-5HT -8 91 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-5HT -8 91 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-5HT -8 91 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-5HT -8 91 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135 2496 38 3H-LSD -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -22 57 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5074 3280 75 3H-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
1574 81 52 125I-LSD -4 20 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 125I-LSD -4 20 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 125I-LSD -4 20 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1809 134 28 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 125I-LSD -218 36 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
180 397 50 3H-5HT -371 38 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-5HT -371 38 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-5HT -371 38 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-5HT -371 38 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-5HT -371 38 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2477 734 54 3H-5HT -61 28 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 734 54 3H-5HT -61 28 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 734 54 3H-5HT -61 28 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 734 54 3H-5HT -61 28 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 734 54 3H-5HT -61 28 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-5HT -457 51 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 2478 19 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -147 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
None 214703 0 UNDEFINED -26 27 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
2726 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-LSD -3 72 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 944 89 3H-LSD -4 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-LSD -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-Risperidone -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-Risperidone -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-Risperidone -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-Risperidone -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-Risperidone -4 91 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10257 728 28 3H-5HT -8 18 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 728 28 3H-5HT -8 18 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 728 28 3H-5HT -8 18 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 728 28 3H-5HT -8 18 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
133 2460 48 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-LSD -91 42 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2337 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
10624 69957 17 3H-LSD -4 32 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69957 17 3H-LSD -4 32 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69957 17 3H-LSD -4 32 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
179 396 107 3H-LSD -134 50 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-LSD -134 50 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-LSD -134 50 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-LSD -134 50 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-LSD -134 50 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
202 1480 0 3H-5HT 1 31 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1480 0 3H-5HT 1 31 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1480 0 3H-5HT 1 31 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1480 0 3H-5HT 1 31 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1480 0 3H-5HT 1 31 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
135398745 2869 108 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -4 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3294 1975 106 3H-LSD -33 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -33 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -33 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -33 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -33 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2389 3279 114 3H-Risperidone -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-Risperidone -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-Risperidone -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-Risperidone -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-Risperidone -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
107 141 116 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-LSD -66 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5074 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2389 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -616 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
115 3732 78 3H-LSD -10 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3732 78 3H-LSD -10 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3732 78 3H-LSD -10 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
24861250 198317 0 UNDEFINED -7 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 None
CHEMBL595252 198317 0 UNDEFINED -7 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 368 5 1 3 4.0 O=S(=O)(c1ccccc1)c1c[nH]c2cccc(CCN3CCCCC3)c12 None
1150 3817 116 125I-LSD -7 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
1150 3817 116 125I-LSD -20 24 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3817 116 125I-LSD -7 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3817 116 125I-LSD -20 24 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3817 116 125I-LSD -7 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3817 116 125I-LSD -20 24 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3817 116 125I-LSD -7 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3817 116 125I-LSD -20 24 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
5074 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 125I-LSD -97 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
11954259 214201 0 3H-LSD -147 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
135 2496 38 125I-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 125I-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 125I-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 125I-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 125I-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1574 81 52 3H-Lysergic 1 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-Lysergic 1 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-Lysergic 1 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
4452 2721 18 3H-LSD -1548 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2721 18 3H-LSD -1548 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2721 18 3H-LSD -1548 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
None 214526 0 3H-LSD -5370 11 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
115 3732 78 125I-LSD -12 26 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3732 78 125I-LSD -12 26 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3732 78 125I-LSD -12 26 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
141 1399 32 3H-LSD -1 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1399 32 3H-LSD -1 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1399 32 3H-LSD -1 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1399 32 3H-LSD -1 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
135398745 2869 108 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5 139 66 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -63 54 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 116 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 125I-LSD -13 30 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
176 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -5 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
66265 93579 12 None 1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93579 12 None 1 19 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
3397 203777 104 None -1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
CHEMBL806 203777 104 None -1 2 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 None
3117 206106 100 None -5 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 206106 100 None -5 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
2543 3651 66 None -194 31 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 None -194 31 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 None -194 31 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 None -194 31 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 None -194 31 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
216239 23591 114 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 23591 114 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 23591 114 None -9 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT6 receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
1353 1880 85 None -1047 85 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -1047 85 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -1047 85 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -1047 85 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -1047 85 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
448537 159703 86 None -35 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159703 86 None -35 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2812 4711 96 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4711 96 None -36 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1588 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3198 203802 73 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203802 73 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203802 73 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
4189 205195 91 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205195 91 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205195 91 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1588 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-5HT -41 43 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
None 214161 0 3H-5HT -141 20 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
3005573 57139 47 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL1655 57139 47 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.2 CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccccc2)cc1 None
2435 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 3533 78 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-LSD -9 48 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-LSD -10 48 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
None 214161 0 3H-5HT -89 20 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 214161 0 3H-5HT -141 20 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1524 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 None -257 51 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5656 201377 82 None 3 40 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201377 82 None 3 40 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
2543 3651 66 None -218 31 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 None -218 31 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 None -218 31 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 None -218 31 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 None -218 31 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 55296 113 None -89 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 None -89 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1548955 88153 17 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
2800 88153 17 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
CHEMBL2355051 88153 17 None -20 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 None
3561 18886 34 None -3 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 18886 34 None -3 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
2470 3596 46 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 None -7413 59 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1209 1628 69 None -46 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 None -46 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 None -46 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 None -46 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 None -46 31 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
2470 3596 46 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 None -7413 59 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
73333 5886 23 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5886 23 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2247 502 77 None -53 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -53 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -53 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -53 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -53 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
4098 32289 24 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1255739 32289 24 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
CHEMBL1411979 32289 24 None -22 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 261 6 0 4 2.7 CN(C)CCN(Cc1cccs1)c1ccccn1 None
2337 3205 72 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 None -54 62 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned 5HT6 receptorBinding affinity to human cloned 5HT6 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
3042 1386 31 None -51 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
355 1386 31 None -51 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
868 1386 31 None -51 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
CHEMBL1123 1386 31 None -51 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
DB00804 1386 31 None -51 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC None
165193 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 None -158 42 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2162 41273 97 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
CHEMBL1491 41273 97 None -2 6 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl None
1201549 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
333 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
7601 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL1201203 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
CHEMBL438151 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
DB00245 590 22 None -77 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 None
3652 4034 72 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4034 72 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4034 72 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4034 72 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4034 72 None -30 18 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1222 1634 44 None -138 32 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1634 44 None -138 32 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1634 44 None -138 32 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1634 44 None -138 32 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1634 44 None -138 32 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2286 3134 48 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 None -26 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
1016 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3690 75 None -38 35 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
3191 102385 93 None -15 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102385 93 None -15 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
191 399 92 3H-LSD -20 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 3H-LSD -20 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 3H-LSD -20 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 3H-LSD -20 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 3H-LSD -20 28 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
133 2460 48 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-LSD -87 42 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 214174 0 3H-5HT -707 59 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135 2496 38 3H-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -22 57 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1880 85 3H-LSD -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-Risperidone -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-Risperidone -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-Risperidone -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-Risperidone -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-Risperidone -2951 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1782 2482 81 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2482 81 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2482 81 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2482 81 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2482 81 3H-LSD -338 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1830 2552 39 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3033769 3229 54 3H-LSD -1380 18 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-LSD -1380 18 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-LSD -1380 18 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-LSD -1380 18 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-LSD -1380 18 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1577 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-LSD -194 25 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
185 3943 54 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
185 3943 54 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-LSD -10715 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-LSD -15488 37 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5567 42556 24 3H-LSD -5495 7 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42556 24 3H-LSD -5495 7 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
54477 84230 34 3H-LSD -69 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-LSD -69 22 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
53389 97995 15 3H-LSD -1 5 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
CHEMBL275707 97995 15 3H-LSD -1 5 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 3.9 C[C@H]1CN(CCCn2c3ccccc3c3ccccc32)C[C@@H](C)N1 None
33630 178379 94 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 3H-LSD -891 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
None 214211 0 3H-LSD 1 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 342 1 1 5 1.8 CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2O)C=C(C=C4)Cl None
None 214212 0 3H-LSD 1 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 334 4 0 3 4.9 C[N+](C)(CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl)[O-] None
1353 1880 85 3H-5HT -346 85 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-5HT -346 85 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-5HT -346 85 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-5HT -346 85 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-5HT -346 85 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
115 3732 78 3H-5HT -12 26 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3732 78 3H-5HT -12 26 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3732 78 3H-5HT -12 26 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2726 906 64 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-5HT -2951 72 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1577 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-LSD -194 25 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
54477 84230 34 3H-LSD -69 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-LSD -69 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2865 4079 67 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
274 3287 39 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
5312145 3287 39 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
CHEMBL433461 3287 39 3H-LSD -1 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N None
134 2478 19 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-LSD -63 67 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1574 81 52 3H-5HT -1 20 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-5HT -1 20 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-5HT -1 20 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
5074 3280 75 3H-LSD -69 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-LSD -69 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-LSD -69 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-LSD -69 29 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2801 161325 56 125I-LSD -6 28 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161325 56 125I-LSD -6 28 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161325 56 125I-LSD -6 28 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
1353 1880 85 3H-LSD -1047 85 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135 2496 38 3H-LSD -21 57 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -21 57 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -21 57 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -21 57 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -21 57 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5 139 66 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -169 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1613 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-5HT -125 54 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1613 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-5HT -5 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1574 81 52 3H-LSD -1 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-LSD -1 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-LSD -1 20 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2543 3651 66 3H-LSD -954 31 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3651 66 3H-LSD -954 31 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3651 66 3H-LSD -954 31 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3651 66 3H-LSD -954 31 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3651 66 3H-LSD -954 31 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
100 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -17 55 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
None 214168 0 3H-LSD -407 23 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6450478 214238 0 3H-LSD -11 11 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
242 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
124087 1362 106 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
7157 1362 106 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
814 1362 106 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
CHEMBL1172 1362 106 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
DB00967 1362 106 None -28 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 None
33630 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 None -13 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
1830 2552 39 None -13 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 None -13 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 None -13 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 None -13 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 None -13 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
191 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
135398745 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
103 4089 56 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -3 53 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2291 3135 52 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3135 52 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3135 52 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3135 52 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3135 52 None -12 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
6075 149575 36 None -13 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
CHEMBL395110 149575 36 None -13 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 None
1209 1628 69 None -12 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 None -12 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 None -12 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 None -12 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 None -12 31 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
124 2933 44 None -100 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2933 44 None -100 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2933 44 None -100 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2933 44 None -100 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2933 44 None -100 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
102 4064 44 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 None -173 49 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2585 790 100 None -109 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 790 100 None -109 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 790 100 None -109 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 790 100 None -109 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 790 100 None -109 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
4211 57517 81 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
CHEMBL1670 57517 81 None 1 4 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 318 3 0 0 5.9 Clc1ccc(C(c2ccccc2Cl)C(Cl)Cl)cc1 None
5323 201101 99 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 None
CHEMBL62193 201101 99 None - 1 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 310 5 2 7 0.9 COc1cc(NS(=O)(=O)c2ccc(N)cc2)nc(OC)n1 None
2600 3720 73 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3720 73 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3720 73 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3720 73 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3720 73 None -5 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
1530 2151 44 None -58 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2151 44 None -58 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2151 44 None -58 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2151 44 None -58 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2151 44 None -58 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
4601 205020 29 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL1201023 205020 29 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
CHEMBL900 205020 29 None -2 17 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 None
135398745 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2351 3234 60 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3234 60 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3234 60 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3234 60 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3234 60 None -10 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
107 141 116 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-5HT -13 30 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
4106 2466 16 3H-5HT -4 33 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-5HT -4 33 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-5HT -4 33 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-5HT -4 33 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
191 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 3H-LSD -7 28 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
100 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
127151 214487 0 None 8 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 313 6 1 4 3.2 CCOC1=CC=CC=C1OC(C2CNCCO2)C3=CC=CC=C3 None
4011 81996 43 None -28 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81996 43 None -28 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
202 1480 0 None 1 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1480 0 None 1 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1480 0 None 1 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1480 0 None 1 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1480 0 None 1 31 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2389 3279 114 None -616 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -616 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -616 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -616 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -616 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 2456 0 None -12 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 None -12 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 None -12 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 None -12 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 None -12 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 944 89 3H-LSD -8 91 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -8 91 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -8 91 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -8 91 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -8 91 Mouse 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
4806 3945 85 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 3945 85 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 3945 85 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 3945 85 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 3945 85 None -13 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT6 receptorBinding affinity to human 5HT6 receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
242 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -144 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
134 2478 19 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -147 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
100 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-LSD -3 55 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2389 3279 114 None -2454 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -2454 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -2454 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -2454 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -2454 67 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
4543 169982 36 None -9 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 None -9 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 None -9 29 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
212 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
10934 1293 111 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
2955 1293 111 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
782 1293 111 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
CHEMBL1043 1293 111 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
DB00250 1293 111 None - 1 Human 8.2 pKi = 8.2 Binding
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 minsAntagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as 5-HT-induced intracellular cAMP production after 30 mins
Drug Central 248 2 2 4 1.7 Nc1ccc(cc1)S(=O)(=O)c1ccc(cc1)N None
5311507 193147 37 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL53904 193147 37 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1 None
5372683 214534 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 400 5 1 4 4.2 C1CN(CCN1CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO None
242 467 117 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -40 51 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
277 1274 55 None -93 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 None -93 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 None -93 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 None -93 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 None -93 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
134 2478 19 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -63 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
49831411 216027 0 None -1 14 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
16106 117643 28 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 None -3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2895 201898 35 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
CHEMBL669 201898 35 None -1 8 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 None
214 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 None -81 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2284 3133 27 None -12 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3133 27 None -12 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3133 27 None -12 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3133 27 None -12 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3133 27 None -12 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
277 1274 55 None -58 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 None -58 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 None -58 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 None -58 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 None -58 45 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1621 2396 16 3H-LSD -17 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-LSD -17 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-LSD -17 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-LSD -17 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-LSD -17 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6971132 214235 0 3H-LSD -1 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
2274 3124 53 None -23 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -23 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -23 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -23 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -23 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2801 161325 56 None -5 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161325 56 None -5 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161325 56 None -5 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
10090005 214210 0 3H-LSD -2 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 361 1 0 3 4.4 CN1CCN(CC1)C2=CC3=C(C=CC(=C3)Cl)C(=CC#N)C4=CC=CC=C42 None
1225 1443 24 None -24 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 None -24 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 None -24 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 None -24 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 None -24 21 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation countingDisplacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
135 2496 38 3H-LSD -22 57 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -22 57 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -22 57 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -22 57 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -22 57 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2865 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1353 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 UNDEFINED -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
133 2460 48 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
133 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5HT -91 42 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2865 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
265 128 0 3H-5HT 4 2 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
89576 128 0 3H-5HT 4 2 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
CHEMBL1288652 128 0 3H-5HT 4 2 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 None
133 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 3H-5HT -87 42 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
3294 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 3596 46 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-5HT -1905 59 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
180 397 50 3H-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
3294 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-LSD -87 44 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1613 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 125I-LSD -5 44 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2337 3205 72 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-LSD -54 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5 139 66 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -169 54 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
180 397 50 3H-LSD -99 38 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -99 38 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -99 38 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -99 38 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -99 38 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
214 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-LSD -79 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-LSD -1047 85 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
73333 5886 23 3H-LSD 1 8 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5886 23 3H-LSD 1 8 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
242 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
141 1399 32 3H-LSD -1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1399 32 3H-LSD -1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1399 32 3H-LSD -1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1399 32 3H-LSD -1 21 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
163839 2910 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 2910 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 2910 0 3H-LSD -36 7 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
107 141 116 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 116 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 116 3H-LSD -66 30 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
180 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
180 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 125I-LSD -154 38 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398745 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 [3H]-LSD -4 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
180 397 50 None -99 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -99 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -99 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -99 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -99 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398737 944 89 3H-LSD -4 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16362 3076 67 None -173 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 None -173 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 None -173 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 None -173 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 None -173 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135 2496 38 None -21 57 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -21 57 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -21 57 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -21 57 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -21 57 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
180 397 50 None -154 38 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -154 38 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -154 38 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -154 38 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -154 38 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
16362 3076 67 None -165 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 None -165 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 None -165 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 None -165 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 None -165 29 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
100 3745 52 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -17 55 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
107715 199260 18 None -17 20 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 199260 18 None -17 20 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 199260 18 None -17 20 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
2865 4079 67 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 None -83 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11978813 713 72 None -8 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 713 72 None -8 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 713 72 None -8 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 713 72 None -8 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 713 72 None -8 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
1588 2294 24 3H-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
6761 67457 17 None -9 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67457 17 None -9 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
191 399 92 None -20 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -20 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -20 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -20 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -20 28 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1588 2294 24 3H-LSD -30 43 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-LSD -30 43 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-LSD -30 43 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-LSD -30 43 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-LSD -30 43 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3294 1975 106 None -87 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 None -87 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 None -87 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 None -87 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 None -87 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
3294 1975 106 None -33 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 None -33 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 None -33 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 None -33 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 None -33 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
133 2460 48 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 None -91 42 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135 2496 38 None -22 57 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -22 57 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -22 57 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -22 57 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -22 57 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
3389 215982 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
26987 936 29 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 936 29 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 936 29 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 936 29 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 936 29 None -58 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2726 906 64 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -10 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1632 45 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -48 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
31101 720 39 None -23 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101 720 39 None -22 35 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 None -23 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 None -22 35 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 None -23 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 None -22 35 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 None -23 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 None -22 35 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 None -23 35 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 None -22 35 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
133 2460 48 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 None -87 42 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2105 3005 34 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 None -31 33 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
209 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
103 4089 56 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-LSD -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
107715 199260 18 None -29 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 199260 18 None -29 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 199260 18 None -29 20 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
2105 3005 34 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 None -19 33 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1212 1632 45 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -26 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1613 2316 44 None -5 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -5 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -5 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -5 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -5 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
209 3008 94 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 None -19 23 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1613 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -4 91 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16106 117643 28 3H-LSD -8 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 117643 28 3H-LSD -8 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
16362 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3076 67 3H-LSD -165 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-LSD -165 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-LSD -165 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-LSD -165 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-LSD -173 29 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-LSD -165 29 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
5281082 214208 0 3H-LSD -30 3 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 411 7 1 6 3.5 CC(=O)C1=CC2=C(C=C1)SC3=CC=CC=C3N2CCCN4CCN(CC4)CCO None
180 397 50 3H-LSD -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1809 134 28 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 3H-LSD -6918 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
71299720 214172 0 125I-LSD -588 16 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
101 3762 18 3H-LSD -120 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3762 18 3H-LSD -120 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3762 18 3H-LSD -120 13 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2865 4079 67 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-LSD -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 UNDEFINED -83 53 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1809 134 28 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 28 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 28 125I-LSD -6918 36 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
145 140 48 3H-Lysergic -7 29 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 3H-Lysergic -7 29 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 3H-Lysergic -7 29 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 3H-Lysergic -7 29 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
242 467 117 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5 139 66 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -125 54 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
145 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 48 125I-LSD -19 29 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
206 2457 10 3H-5HT -1995 24 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2457 10 3H-5HT -1995 24 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2457 10 3H-5HT -1995 24 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
124936 215955 0 3H-LSD -3 7 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 268 3 1 5 4.8 CNC1=CC=C(C=C1)N=NC2=CC3=C(C=C2)N=CS3 None
135398745 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -4 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
134551 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 355 25 None -6 21 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
1588 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1588 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 125I-LSD -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
191 399 92 None -7 28 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -7 28 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -7 28 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -7 28 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -7 28 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
100 3745 52 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -3 55 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1588 2294 24 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 None -30 43 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2435 3533 78 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 None -9 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cellsDisplacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
10531 1392 18 None -21 24 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1392 18 None -21 24 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1392 18 None -21 24 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1392 18 None -21 24 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1392 18 None -21 24 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
1588 2294 24 None -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 None -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 None -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 None -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 None -41 43 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
103 4089 56 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -3 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -3 72 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 944 89 None -4 91 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -4 91 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -4 91 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -4 91 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -4 91 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1621 2396 16 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11976 907 54 None -3 23 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 None -3 23 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 None -3 23 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 None -3 23 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptorBinding affinity towards human 5-hydroxytryptamine 6 receptor
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135398745 2869 108 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -4 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954224 214174 0 None -141 59 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214174 0 None -181 59 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1238 201484 21 None -5 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 None -5 16 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
1621 2396 16 None -17 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 None -17 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 None -17 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 None -17 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 None -17 44 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1042 1551 20 None -5 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1551 20 None -5 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1551 20 None -5 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1551 20 None -5 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1551 20 None -5 16 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
10531 1392 18 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1392 18 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1392 18 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1392 18 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1392 18 None -9 24 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
103 4089 56 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -1 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
150 2473 18 None -2 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2473 18 None -2 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2473 18 None -2 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2473 18 None -2 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2473 18 None -2 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
None 214177 0 125I-LSD -107 6 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
180 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135 2496 38 3H-LSD -21 57 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-LSD -21 57 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-LSD -21 57 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-LSD -21 57 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-LSD -21 57 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
180 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-5HT -154 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
242 467 117 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-LSD -144 51 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
180 397 50 3H-LSD -371 38 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-LSD -371 38 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-LSD -371 38 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-LSD -371 38 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-LSD -371 38 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
46780481 107045 18 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 None -8 53 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
135409468 2004 63 3H-LSD -3 40 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-LSD -3 40 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-LSD -3 40 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
135398737 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-LSD -4 91 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3337 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-LSD -117 40 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
5 139 66 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-LSD -63 54 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
101 3762 18 3H-LSD -1548 13 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 3762 18 3H-LSD -1548 13 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 3762 18 3H-LSD -1548 13 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
2389 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-LSD -2454 67 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11256720 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
9444 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
CHEMBL1083390 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
DB12680 2024 73 None -1 6 Human 9.8 pKi = 9.8 Binding
HeLa cell membrane assay, displacing [<sup>3</sup>H]LSDHeLa cell membrane assay, displacing [<sup>3</sup>H]LSD
Guide to Pharmacology 353 3 1 5 2.5 O=S(=O)(c1cnc2c(c1)cccc2N1CCNCC1)c1ccccc1 24878269
4806 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 3945 85 None -13 13 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
242 467 117 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
34 467 117 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
60795 467 117 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
CHEMBL1112 467 117 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
DB01238 467 117 None -40 51 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10327430
275 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
275 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
3246 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
5312144 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL46071 3308 6 None -1 2 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
10337743 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
8429 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
CHEMBL571858 4013 16 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 347 5 0 5 2.6 CN(CCn1cc(c2c1nccc2)S(=O)(=O)c1cccc(c1)F)C 19523834
3235 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
6918553 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
CHEMBL329383 3464 12 None - 1 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 521 5 2 5 3.6 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Br)cc(c1Br)F 11140733
3232 3453 13 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
3248571 3453 13 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
CHEMBL60264 3453 13 None 2 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 487 5 1 5 2.9 COc1ccc(cc1N1CCN(CC1)C)NS(=O)(=O)c1ccc(cc1)I 10928963
10202564 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
3217 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
CHEMBL362628 1496 8 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 423 6 2 6 3.4 CN(CCc1c[nH]c2c1cc(cc2)NS(=O)(=O)c1c(Cl)nc2n1ccs2)C 15771424
10150497 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
3240 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
CHEMBL392760 4011 41 None 60 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 4 1 7 2.7 NCCc1cn(c2c1cccc2)S(=O)(=O)c1c(Cl)nc2n1ccs2 17625499
16071605 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
7356 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
CHEMBL2103880 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
DB12229 867 22 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 5 3.9 CN(CCCOc1ccc2c(c1)c([nH]n2)S(=O)(=O)c1cccc2c1cccc2)C None
276 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
5312149 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
CHEMBL431298 3457 45 None 81 13 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 9925723
3241 3465 17 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
6918649 3465 17 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
CHEMBL1210710 3465 17 None - 1 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 6 2 6 3.2 COc1ccc(cc1N1CCNCC1)S(=O)(=O)Nc1cc(Cl)cc(c1OC)Cl 17069795
21071390 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
8689 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
CHEMBL3286580 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
DB11957 1956 48 None -2 7 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 398 9 2 2 4.9 Fc1ccc2c(c1)[nH]cc2CCNCc1cccc(c1)OCC(C(F)F)(F)F 24878269
3337 214441 0 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 None -117 40 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
179 396 107 None -134 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 None -134 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 None -134 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 None -134 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 None -134 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2543 3651 66 None -194 31 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
5358 3651 66 None -194 31 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
54 3651 66 None -194 31 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
CHEMBL128 3651 66 None -194 31 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
DB00669 3651 66 None -194 31 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
206 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
206 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
206 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
68848 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
68848 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
68848 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
CHEMBL12314 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 7680751
CHEMBL12314 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9225298
CHEMBL12314 2457 10 None -1995 24 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
152 361 18 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
2107 361 18 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
CHEMBL275854 361 18 None -416 18 Rat 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 9798944
206 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
206 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
206 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
68848 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
68848 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
68848 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
CHEMBL12314 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 8522988
CHEMBL12314 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9284367
CHEMBL12314 2457 10 None -1318 24 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 9730917
29 780 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 780 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 780 0 None -3981 9 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
197706 1436 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1436 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1436 0 None -12589 10 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
1355 1980 82 None -158 15 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
142 1980 82 None -158 15 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
CHEMBL478 1980 82 None -158 15 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
DB12110 1980 82 None -158 15 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 7680751
2389 3279 114 None -2454 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
5073 3279 114 None -2454 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
96 3279 114 None -2454 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
CHEMBL85 3279 114 None -2454 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
DB00734 3279 114 None -2454 67 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8522988
2543 3651 66 None -218 31 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
5358 3651 66 None -218 31 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
54 3651 66 None -218 31 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
CHEMBL128 3651 66 None -218 31 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
DB00669 3651 66 None -218 31 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8522988
1209 1628 69 None -46 31 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
203 1628 69 None -46 31 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
3386 1628 69 None -46 31 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
CHEMBL41 1628 69 None -46 31 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
DB00472 1628 69 None -46 31 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 7680751
107780 1814 50 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 1814 50 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 1814 50 None -3162 17 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
2470 3596 46 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
3300 3596 46 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
5265 3596 46 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
99 3596 46 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
CHEMBL267930 3596 46 None -7413 59 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7908055
10 715 23 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 715 23 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 715 23 None -100 9 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3652 4034 72 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4034 72 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4034 72 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4034 72 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4034 72 None -30 18 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
101 3762 18 None -1548 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
55752 3762 18 None -1548 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
CHEMBL35057 3762 18 None -1548 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 8522988
1809 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
1809 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
1809 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
4 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
4 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
4 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
CHEMBL18840 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7680751
CHEMBL18840 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9225298
CHEMBL18840 134 28 None -6918 36 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 9798944
1809 134 28 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
4 134 28 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
CHEMBL18840 134 28 None -6918 36 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8522988
109 889 23 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
2689 889 23 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
CHEMBL27403 889 23 None -281 7 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 7680751
121930 2364 29 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
18 2364 29 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
CHEMBL1256693 2364 29 None -630 2 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 349 4 1 3 3.7 Nc1ccc(cc1)CCN1CCN(CC1)c1cccc(c1)C(F)(F)F 7680751
2389 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
2389 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
5073 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
5073 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
96 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
96 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
CHEMBL85 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
CHEMBL85 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
DB00734 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 7908055
DB00734 3279 114 None -616 67 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8997630
163839 2910 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
268 2910 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
CHEMBL55171 2910 0 None -36 7 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 10327430
108029 3361 50 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
23 3361 50 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
CHEMBL18785 3361 50 None -630 13 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8522988
1150 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
1150 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
125 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
125 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
CHEMBL6640 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
CHEMBL6640 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
DB08653 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 7680751
DB08653 3817 116 None -20 24 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 9225298
115 3732 78 None -12 26 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
4296 3732 78 None -12 26 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
CHEMBL274866 3732 78 None -12 26 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 7680751
202 1480 0 None 1 31 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
60835 1480 0 None 1 31 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
972 1480 0 None 1 31 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
CHEMBL1175 1480 0 None 1 31 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
DB00476 1480 0 None 1 31 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 11750180
115 3732 78 None -10 26 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
4296 3732 78 None -10 26 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
CHEMBL274866 3732 78 None -10 26 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8522988
134 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
134 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
134 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
134 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
1775 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
1775 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
1775 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1775 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
9681 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
9681 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
9681 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
9681 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
CHEMBL1065 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
CHEMBL1065 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
CHEMBL1065 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
CHEMBL1065 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
DB00247 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7680751
DB00247 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9225298
DB00247 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
DB00247 2478 19 None -147 67 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9798944
267 1419 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
9847259 1419 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
CHEMBL4214961 1419 0 None -1 2 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 5 4.6 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1ccc(c(c1Cl)Cl)O 10327430
134 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
134 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
134 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1775 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
1775 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
1775 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
9681 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
9681 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
9681 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
CHEMBL1065 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
CHEMBL1065 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
CHEMBL1065 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
DB00247 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8522988
DB00247 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9284367
DB00247 2478 19 None -63 67 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 9730917
1574 81 52 None -1 20 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
218 81 52 None -1 20 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
CHEMBL266591 81 52 None -1 20 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 9225298
277 1274 55 None -93 45 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
2913 1274 55 None -93 45 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
765 1274 55 None -93 45 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
CHEMBL516 1274 55 None -93 45 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
DB00434 1274 55 None -93 45 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 8522988
265 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
265 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
265 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
89576 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
89576 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
89576 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
CHEMBL1288652 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 7680751
CHEMBL1288652 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9225298
CHEMBL1288652 128 0 None 4 2 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 5 2 2 3.2 NCCc1c[nH]c2c1cc(OCc1ccccc1)cc2 9798944
180 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
180 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
180 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
200 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
200 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
200 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
2160 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
2160 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
2160 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
CHEMBL629 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
CHEMBL629 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
CHEMBL629 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
DB00321 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 7680751
DB00321 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9225298
DB00321 397 50 None -154 38 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
133 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
133 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
133 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
1723 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
1723 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
1723 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
28693 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
28693 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
28693 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
CHEMBL19215 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
CHEMBL19215 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
CHEMBL19215 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
DB13520 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8522988
DB13520 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9284367
DB13520 2460 48 None -91 42 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
145 140 48 None -19 29 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
1832 140 48 None -19 29 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
CHEMBL7257 140 48 None -19 29 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
DB14010 140 48 None -19 29 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 9798944
277 1274 55 None -58 45 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
2913 1274 55 None -58 45 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
765 1274 55 None -58 45 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
CHEMBL516 1274 55 None -58 45 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
DB00434 1274 55 None -58 45 Rat 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 7680751
1342 36 42 None -42 18 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
3 36 42 None -42 18 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
CHEMBL277120 36 42 None -42 18 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 7680751
133 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
133 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
133 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
133 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
1723 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
1723 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
1723 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
1723 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
28693 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
28693 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
28693 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
28693 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
CHEMBL19215 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
CHEMBL19215 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
CHEMBL19215 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
CHEMBL19215 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
DB13520 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7680751
DB13520 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9225298
DB13520 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9730917
DB13520 2460 48 None -87 42 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 9798944
180 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
180 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
180 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
200 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
200 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
200 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
2160 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
2160 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
2160 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
CHEMBL629 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
CHEMBL629 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
CHEMBL629 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
DB00321 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 8522988
DB00321 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9284367
DB00321 397 50 None -99 38 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 9730917
135 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
135 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
135 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
1796 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
1796 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
1796 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
4184 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
4184 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
4184 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
CHEMBL6437 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
CHEMBL6437 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
CHEMBL6437 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
DB06148 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 8522988
DB06148 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9284367
DB06148 2496 38 None -21 57 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
209 3008 94 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
2113 3008 94 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
4748 3008 94 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
CHEMBL567 3008 94 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
DB00850 3008 94 None -30 23 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 15821958
101 3762 18 None -120 13 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
55752 3762 18 None -120 13 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
CHEMBL35057 3762 18 None -120 13 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 7908055
5074 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
5074 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
5074 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
5074 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
97 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
97 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
97 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
97 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
CHEMBL267777 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
CHEMBL267777 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
CHEMBL267777 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
CHEMBL267777 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
DB12693 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 7680751
DB12693 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9225298
DB12693 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
DB12693 3280 75 None -97 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9798944
5 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
5 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
5 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5202 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
5202 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
5202 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
CHEMBL39 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
CHEMBL39 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
CHEMBL39 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
DB08839 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8522988
DB08839 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9284367
DB08839 139 66 None -169 54 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
135 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
135 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
135 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
1796 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
1796 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
1796 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
4184 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
4184 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
4184 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
CHEMBL6437 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
CHEMBL6437 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
CHEMBL6437 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
DB06148 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 7680751
DB06148 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9225298
DB06148 2496 38 None -22 57 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 9730917
5074 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
5074 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
5074 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
97 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
97 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
97 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
CHEMBL267777 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
CHEMBL267777 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
CHEMBL267777 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
DB12693 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 8522988
DB12693 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9284367
DB12693 3280 75 None -69 29 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9730917
278 1390 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
3065 1390 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
CHEMBL1967279 1390 0 None - 1 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 611 5 3 6 2.7 CN1CC(CC2C1Cc1c[nH]c3c1c2ccc3)C(=O)NC1(OC2(N(C1=O)C(Cc1ccccc1)C(=O)N1C2CCC1)O)C(C)C 9798944
141 1399 32 None -1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
6089 1399 32 None -1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
CHEMBL12420 1399 32 None -1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
DB01488 1399 32 None -1 21 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 8522988
3294 1975 106 None -87 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
71360 1975 106 None -87 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
87 1975 106 None -87 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
CHEMBL14376 1975 106 None -87 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
DB04946 1975 106 None -87 44 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 11750183
16362 3076 67 None -165 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
2172 3076 67 None -165 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
90 3076 67 None -165 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
CHEMBL1423 3076 67 None -165 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
DB01100 3076 67 None -165 29 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 7908055
100 3745 52 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
2637 3745 52 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
5452 3745 52 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
CHEMBL479 3745 52 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
DB00679 3745 52 None -17 55 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 15821958
5 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
5 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
5202 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
5202 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
5202 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
5202 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
CHEMBL39 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
CHEMBL39 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
CHEMBL39 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
CHEMBL39 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
DB08839 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7680751
DB08839 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9225298
DB08839 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9730917
DB08839 139 66 None -125 54 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9798944
134551 355 25 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
271 355 25 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
885 355 25 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
CHEMBL1403281 355 25 None -38 21 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C 9798944
191 399 92 None -20 28 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
201 399 92 None -20 28 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
2170 399 92 None -20 28 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
CHEMBL1113 399 92 None -20 28 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
DB00543 399 92 None -20 28 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 8522988
1212 1632 45 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
204 1632 45 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
3372 1632 45 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
CHEMBL726 1632 45 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
DB00623 1632 45 None -48 65 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 15821958
279 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
279 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
49381 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
49381 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
CHEMBL63756 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 15821958
CHEMBL63756 1631 26 None -7 17 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 8522988
107 141 116 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
1833 141 116 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
CHEMBL8165 141 116 None -66 30 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8522988
3294 1975 106 None -33 44 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
71360 1975 106 None -33 44 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
87 1975 106 None -33 44 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
CHEMBL14376 1975 106 None -33 44 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
DB04946 1975 106 None -33 44 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 8997630
270 2262 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
6918447 2262 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
CHEMBL80937 2262 0 None - 1 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 299 1 1 2 3.7 N#CC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c([nH]3)Cl 7680751
1613 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
1613 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
205 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
205 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
3964 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
3964 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
CHEMBL831 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
CHEMBL831 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
DB00408 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7680751
DB00408 2316 44 None -5 44 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 7908055
1613 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
1613 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
205 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
205 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
3964 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
3964 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
CHEMBL831 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
CHEMBL831 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
DB00408 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 15821958
DB00408 2316 44 None -4 44 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 8522988
274 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
274 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
5312145 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
5312145 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL433461 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL433461 3287 39 None 1 3 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
31101 720 39 None -23 35 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
31101 720 39 None -22 35 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
35 720 39 None -23 35 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
35 720 39 None -22 35 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
403 720 39 None -23 35 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
403 720 39 None -22 35 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
CHEMBL493 720 39 None -23 35 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
CHEMBL493 720 39 None -22 35 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
DB01200 720 39 None -23 35 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 8522988
DB01200 720 39 None -22 35 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 9798944
2105 3005 34 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
47811 3005 34 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
48 3005 34 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
CHEMBL531 3005 34 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
DB01186 3005 34 None -31 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 7680751
274 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
274 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
5312145 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
5312145 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL433461 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL433461 3287 39 None -1 3 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 4 7 0.9 CNc1nc(NC)nc(c1)NS(=O)(=O)c1ccc(cc1)N 9730917
167 3376 0 None -25 5 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
9821498 3376 0 None -25 5 Rat 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 385 7 0 5 3.6 Fc1ccc(cc1)C(=O)CC1CCN(C1)CCOc1cccc2c1OCCO2 9732398
107 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
107 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
107 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
1833 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
1833 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
1833 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
CHEMBL8165 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 7680751
CHEMBL8165 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9225298
CHEMBL8165 141 116 None -35 30 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 9798944
10257 728 28 None -8 18 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
144 728 28 None -8 18 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
CHEMBL416526 728 28 None -8 18 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
DB01445 728 28 None -8 18 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 9225298
6918515 2574 33 None 4 6 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
71 2574 33 None 4 6 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
CHEMBL7318 2574 33 None 4 6 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
2726 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2726 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
621 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
621 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
83 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
83 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
CHEMBL71 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
CHEMBL71 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
DB00477 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 15821958
DB00477 906 64 None -10 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8522988
1043 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
1043 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
1043 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
149 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
149 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
149 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
8223 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
8223 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
8223 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
CHEMBL442 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
CHEMBL442 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
CHEMBL442 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
DB00696 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9225298
DB00696 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
DB00696 1552 13 None -173 28 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
10171 57 15 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
272 57 15 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
CHEMBL274384 57 15 None -7 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 7680751
12 1524 14 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918513 1524 14 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
CHEMBL267615 1524 14 None 6 7 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
279 1631 26 None -3 17 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
49381 1631 26 None -3 17 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
CHEMBL63756 1631 26 None -3 17 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 7908055
1212 1632 45 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
204 1632 45 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
3372 1632 45 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
CHEMBL726 1632 45 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
DB00623 1632 45 None -26 65 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7908055
209 3008 94 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
2113 3008 94 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
4748 3008 94 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
CHEMBL567 3008 94 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
DB00850 3008 94 None -19 23 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 7908055
191 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
191 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
201 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
201 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
2170 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
2170 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
CHEMBL1113 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
CHEMBL1113 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
DB00543 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7680751
DB00543 399 92 None -7 28 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 7908055
1588 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
1588 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
1588 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
1588 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
28864 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
28864 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
28864 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
28864 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
43 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
43 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
43 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
43 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
CHEMBL157138 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
CHEMBL157138 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
CHEMBL157138 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL157138 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
DB00589 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 7680751
DB00589 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
DB00589 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB00589 2294 24 None -41 43 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9798944
275 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
275 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
3246 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
3246 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
5312144 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
5312144 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
CHEMBL46071 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9647481
CHEMBL46071 3308 6 None 1 2 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 5 4 6 1.5 CNc1cc(cc(n1)NC)NS(=O)(=O)c1ccc(cc1)N 9730917
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
135398737 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
38 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
722 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
CHEMBL42 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7680751
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7908055
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8997630
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9225298
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9732398
DB00363 944 89 None -4 91 Rat 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9798944
135398737 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
135398737 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
135398737 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
135398737 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
38 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
38 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
38 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
38 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
722 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
722 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
722 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
722 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
CHEMBL42 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
CHEMBL42 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
CHEMBL42 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
CHEMBL42 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
DB00363 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 15821958
DB00363 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8522988
DB00363 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9284367
DB00363 944 89 None -4 91 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 9730917
122265 1944 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
273 1944 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
CHEMBL1191534 1944 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 5 0 3 4.6 CN(CCSc1nc2ccccc2cc1c1ccccc1)C 8522988
135398745 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
135398745 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
47 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
47 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
CHEMBL715 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
DB00334 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 15821958
DB00334 2869 108 None -4 65 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8522988
1588 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
1588 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
28864 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
28864 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
43 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
43 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL157138 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
CHEMBL157138 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB00589 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9284367
DB00589 2294 24 None -30 43 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
135398745 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
135398745 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
47 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
47 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
CHEMBL715 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
CHEMBL715 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
DB00334 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 7908055
DB00334 2869 108 None -4 65 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8997630
10531 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
10531 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
121 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
121 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
888 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
888 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
CHEMBL1732 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
CHEMBL1732 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
DB00320 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7680751
DB00320 1392 18 None -21 24 Rat 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9798944
100 3745 52 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
2637 3745 52 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
5452 3745 52 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
CHEMBL479 3745 52 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
DB00679 3745 52 None -3 55 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 7908055
1621 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
1621 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
17 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
17 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
5761 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
5761 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL263881 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
CHEMBL263881 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB04829 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9225298
DB04829 2396 16 None -17 44 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
1043 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
1043 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
149 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
149 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
8223 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
8223 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
CHEMBL442 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
CHEMBL442 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
DB00696 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9284367
DB00696 1552 13 None -23 28 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 9730917
103 4089 56 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2875 4089 56 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
5736 4089 56 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
CHEMBL285802 4089 56 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
DB09225 4089 56 None -3 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 15821958
2726 906 64 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
621 906 64 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
83 906 64 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
CHEMBL71 906 64 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
DB00477 906 64 None -3 72 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 7908055
1621 2396 16 None -16 44 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
17 2396 16 None -16 44 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
5761 2396 16 None -16 44 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
CHEMBL263881 2396 16 None -16 44 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
DB04829 2396 16 None -16 44 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 9730917
4106 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
4106 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
4106 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
4106 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
5358812 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
5358812 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
5358812 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
5358812 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
89 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
89 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
89 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
89 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
CHEMBL93240 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7680751
CHEMBL93240 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9225298
CHEMBL93240 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
CHEMBL93240 2466 16 None -7 33 Rat 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9798944
4106 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
4106 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
4106 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
5358812 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
5358812 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
5358812 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
89 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
89 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
89 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
CHEMBL93240 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8522988
CHEMBL93240 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9284367
CHEMBL93240 2466 16 None -1 33 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 9730917
103 4089 56 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
2875 4089 56 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
5736 4089 56 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
CHEMBL285802 4089 56 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055
DB09225 4089 56 None -1 53 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 7908055